Identification

Generic Name
ATP
DrugBank Accession Number
DB00171
Background

An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.

Type
Small Molecule
Groups
Investigational, Nutraceutical
Structure
Weight
Average: 507.181
Monoisotopic: 506.995745159
Chemical Formula
C10H16N5O13P3
Synonyms
  • Adenosine 5'-triphosphate
  • Adenosine triphosphate
  • Adenosine-5'-triphosphate
  • ATP

Pharmacology

Indication

For nutritional supplementation, also for treating dietary shortage or imbalance

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofArrhythmia supraventricular•••••••••••••••••••••
Treatment ofSupraventricular arrhythmias••••••••••••••••••• •••• ••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Adenosine triphosphate (ATP) is the nucleotide known in biochemistry as the "molecular currency" of intracellular energy transfer; that is, ATP is able to store and transport chemical energy within cells. ATP also plays an important role in the synthesis of nucleic acids. The total quantity of ATP in the human body is about 0.1 mole. The energy used by human cells requires the hydrolysis of 200 to 300 moles of ATP daily. This means that each ATP molecule is recycled 2000 to 3000 times during a single day. ATP cannot be stored, hence its consumption must closely follow its synthesis.

Mechanism of action

ATP is able to store and transport chemical energy within cells. ATP also plays an important role in the synthesis of nucleic acids. ATP can be produced by various cellular processes, most typically in mitochondria by oxidative phosphorylation under the catalytic influence of ATP synthase. The total quantity of ATP in the human body is about 0.1 mole. The energy used by human cells requires the hydrolysis of 200 to 300 moles of ATP daily. This means that each ATP molecule is recycled 2000 to 3000 times during a single day. ATP cannot be stored, hence its consumption must closely follow its synthesis.

TargetActionsOrganism
UMultidrug resistance-associated protein 6Not AvailableHumans
UMultidrug resistance-associated protein 4Not AvailableHumans
UMultidrug resistance-associated protein 1Not AvailableHumans
UCystic fibrosis transmembrane conductance regulator
cofactor
Humans
UPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformNot AvailableHumans
UCasein kinase II subunit alphaNot AvailableHumans
UCasein kinase II subunit betaNot AvailableHumans
UP2Y purinoceptor 11Not AvailableHumans
USerine/threonine-protein phosphatase 5Not AvailableHumans
UTyrosine-protein kinase ABL2
inhibitor
Humans
UATP-binding cassette sub-family A member 1Not AvailableHumans
UAcetyl-coenzyme A synthetase, cytoplasmicNot AvailableHumans
UALK tyrosine kinase receptorNot AvailableHumans
UNEDD8-activating enzyme E1 regulatory subunitNot AvailableHumans
U5'-AMP-activated protein kinase catalytic subunit alpha-1Not AvailableHumans
USerine/threonine-protein kinase A-RafNot AvailableHumans
USerine/threonine-protein kinase receptor R3Not AvailableHumans
ULong-chain-fatty-acid--CoA ligase 1Not AvailableHumans
UCytosolic purine 5'-nucleotidaseNot AvailableHumans
UATPase ASNA1Not AvailableHumans
UATP-binding cassette sub-family C member 9Not AvailableHumans
URAC-alpha serine/threonine-protein kinaseNot AvailableHumans
UBeta-adrenergic receptor kinase 1Not AvailableHumans
UApoptotic protease-activating factor 1Not AvailableHumans
UAcetyl-coenzyme A synthetase 2-like, mitochondrialNot AvailableHumans
UActivin receptor type-1BNot AvailableHumans
UActivin receptor type-1Not AvailableHumans
UBile salt export pumpNot AvailableHumans
UAsparagine synthetase [glutamine-hydrolyzing]Not AvailableHumans
UCyclin-dependent kinase 15Not AvailableHumans
UADP/ATP translocase 1Not AvailableHumans
UATP-binding cassette sub-family C member 8Not AvailableHumans
UArgininosuccinate synthaseNot AvailableHumans
UAFG3-like protein 2Not AvailableHumans
UBeta-adrenergic receptor kinase 2Not AvailableHumans
UAnti-Muellerian hormone type-2 receptorNot AvailableHumans
UActivated CDC42 kinase 1Not AvailableHumans
UTyrosine-protein kinase ABL1
inhibitor
Humans
UAdenylate cyclase type 1Not AvailableHumans
UP-glycoprotein 1Not AvailableHumans
UATP-binding cassette sub-family G member 1Not AvailableHumans
UCanalicular multispecific organic anion transporter 1Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Oral LD50 in rats is > 2 g/kg.

Pathways
PathwayCategory
Carbamoyl Phosphate Synthetase DeficiencyDisease
Argininosuccinic AciduriaDisease
Glycine and Serine MetabolismMetabolic
Ammonia RecyclingMetabolic
Inositol MetabolismMetabolic
Propanoate MetabolismMetabolic
Arginine and Proline MetabolismMetabolic
Selenoamino Acid MetabolismMetabolic
Pentose Phosphate PathwayMetabolic
Glycerolipid MetabolismMetabolic
Galactose MetabolismMetabolic
Histidine MetabolismMetabolic
Pyrimidine MetabolismMetabolic
Purine MetabolismMetabolic
Fatty Acid MetabolismMetabolic
Citric Acid CycleMetabolic
Starch and Sucrose MetabolismMetabolic
Pyruvate MetabolismMetabolic
Glutamate MetabolismMetabolic
Butyrate MetabolismMetabolic
Thiamine MetabolismMetabolic
Simvastatin Action PathwayDrug action
Pravastatin Action PathwayDrug action
Rosuvastatin Action PathwayDrug action
Zoledronate Action PathwayDrug action
Pamidronate Action PathwayDrug action
Fluvastatin Action PathwayDrug action
Betaine MetabolismMetabolic
GluconeogenesisMetabolic
2-Methyl-3-hydroxybutryl-CoA Dehydrogenase DeficiencyDisease
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Adenosine triphosphate disodium5L51B4DR1G987-65-5TTWYZDPBDWHJOR-IDIVVRGQSA-L
Adenosine triphosphate disodium trihydrate7ZRM409FOZ51963-61-2MWEQTWJABOLLOS-AZGWGOJFSA-L
International/Other Brands
Atriphos (Biochimica) / Striadyne (Auclair)

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as purine ribonucleoside triphosphates. These are purine ribobucleotides with a triphosphate group linked to the ribose moiety.
Kingdom
Organic compounds
Super Class
Nucleosides, nucleotides, and analogues
Class
Purine nucleotides
Sub Class
Purine ribonucleotides
Direct Parent
Purine ribonucleoside triphosphates
Alternative Parents
Purine ribonucleoside monophosphates / Pentose phosphates / Glycosylamines / 6-aminopurines / Monosaccharide phosphates / Monoalkyl phosphates / Aminopyrimidines and derivatives / N-substituted imidazoles / Imidolactams / Heteroaromatic compounds
show 9 more
Substituents
1,2-diol / 6-aminopurine / Alcohol / Alkyl phosphate / Amine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Azole / Glycosyl compound
show 30 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
adenosine 5'-phosphate, purine ribonucleoside 5'-triphosphate (CHEBI:15422) / Ribonucleotides, Coenzymes (C00002)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
8L70Q75FXE
CAS number
56-65-5
InChI Key
ZKHQWZAMYRWXGA-KQYNXXCUSA-N
InChI
InChI=1S/C10H16N5O13P3/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(17)6(16)4(26-10)1-25-30(21,22)28-31(23,24)27-29(18,19)20/h2-4,6-7,10,16-17H,1H2,(H,21,22)(H,23,24)(H2,11,12,13)(H2,18,19,20)/t4-,6-,7-,10-/m1/s1
IUPAC Name
({[({[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy](hydroxy)phosphoryl}oxy)phosphonic acid
SMILES
NC1=NC=NC2=C1N=CN2[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O

References

Synthesis Reference

George M. Whitesides, Patricia E. Garrett, Merrell G. Siegel, "Method for preparing adenosine triphosphate." U.S. Patent US4164444, issued April, 1975.

US4164444
General References
  1. Gajewski E, Steckler DK, Goldberg RN: Thermodynamics of the hydrolysis of adenosine 5'-triphosphate to adenosine 5'-diphosphate. J Biol Chem. 1986 Sep 25;261(27):12733-7. [Article]
  2. Storer AC, Cornish-Bowden A: Concentration of MgATP2- and other ions in solution. Calculation of the true concentrations of species present in mixtures of associating ions. Biochem J. 1976 Oct 1;159(1):1-5. [Article]
  3. Wilson JE, Chin A: Chelation of divalent cations by ATP, studied by titration calorimetry. Anal Biochem. 1991 Feb 15;193(1):16-9. [Article]
  4. Garfinkel L, Altschuld RA, Garfinkel D: Magnesium in cardiac energy metabolism. J Mol Cell Cardiol. 1986 Oct;18(10):1003-13. [Article]
  5. Parsons M: Glycosomes: parasites and the divergence of peroxisomal purpose. Mol Microbiol. 2004 Aug;53(3):717-24. [Article]
Human Metabolome Database
HMDB0000538
KEGG Drug
D08646
KEGG Compound
C00002
PubChem Compound
5957
PubChem Substance
46507614
ChemSpider
5742
BindingDB
2
RxNav
318
ChEBI
15422
ChEMBL
CHEMBL14249
ZINC
ZINC000004261765
Therapeutic Targets Database
DNC000262
PharmGKB
PA164743471
PDBe Ligand
ATP
Wikipedia
Adenosine_triphosphate
PDB Entries
1a0i / 1a49 / 1a5u / 1a82 / 1aq2 / 1asz / 1atn / 1atp / 1ayl / 1b0u
show 2491 more
MSDS
Download (72.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAtrial Fibrillation1
3CompletedTreatmentCancer / Palliative Treatment / Quality of Life (QOL) / Survival1
2CompletedOtherAlzheimer's Disease (AD)1
2Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
1CompletedBasic ScienceChronic Heart Failure (CHF)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)176 °CNot Available
water solubility1E+006 mg/LMERCK INDEX (1996); freely soluble
logP-5.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.49 mg/mLALOGPS
logP-0.84ALOGPS
logP-5.4Chemaxon
logS-2ALOGPS
pKa (Strongest Acidic)0.9Chemaxon
pKa (Strongest Basic)4.93Chemaxon
Physiological Charge-4Chemaxon
Hydrogen Acceptor Count14Chemaxon
Hydrogen Donor Count7Chemaxon
Polar Surface Area279.13 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity95.81 m3·mol-1Chemaxon
Polarizability39.07 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.8672
Blood Brain Barrier+0.9035
Caco-2 permeable-0.7475
P-glycoprotein substrateNon-substrate0.6692
P-glycoprotein inhibitor INon-inhibitor0.8983
P-glycoprotein inhibitor IINon-inhibitor0.9763
Renal organic cation transporterNon-inhibitor0.9571
CYP450 2C9 substrateNon-substrate0.8379
CYP450 2D6 substrateNon-substrate0.8363
CYP450 3A4 substrateNon-substrate0.5673
CYP450 1A2 substrateNon-inhibitor0.8908
CYP450 2C9 inhibitorNon-inhibitor0.9403
CYP450 2D6 inhibitorNon-inhibitor0.9005
CYP450 2C19 inhibitorNon-inhibitor0.9352
CYP450 3A4 inhibitorNon-inhibitor0.9375
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.976
Ames testNon AMES toxic0.8933
CarcinogenicityNon-carcinogens0.9165
BiodegradationNot ready biodegradable0.9645
Rat acute toxicity2.5022 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9727
hERG inhibition (predictor II)Non-inhibitor0.8159
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-004j-9785600000-9d385d54b8bf3d01c79a
LC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , NegativeLC-MS/MSsplash10-0a4i-0131190000-316dbdca27f38ad8ee57
LC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , NegativeLC-MS/MSsplash10-004i-0000900000-f5ffc4694dfd302fd52d
LC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , NegativeLC-MS/MSsplash10-0a4i-0000900000-e9a09b9360491c310280
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0000900000-f5ffc4694dfd302fd52d
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0a4i-0000900000-e9a09b9360491c310280
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4i-0000090000-97853f04c0eb7ec8c18b
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-0000090000-17d473bc9ec2a72bd4f3
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udj-0059330000-729b4b2c718850c360f3
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a6r-3211940000-161d1056f6495ab27eca
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0007-0902000000-34fc3024c68745188ff6
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-056r-5900800000-caf5da3be97f3b8e030b
13C NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-219.8533928
predicted
DarkChem Lite v0.1.0
[M-H]-225.8660928
predicted
DarkChem Lite v0.1.0
[M-H]-205.0044928
predicted
DarkChem Lite v0.1.0
[M-H]-231.7764928
predicted
DarkChem Lite v0.1.0
[M-H]-168.8962
predicted
DeepCCS 1.0 (2019)
[M+H]+223.1981928
predicted
DarkChem Lite v0.1.0
[M+H]+225.5127928
predicted
DarkChem Lite v0.1.0
[M+H]+206.0154928
predicted
DarkChem Lite v0.1.0
[M+H]+230.7223928
predicted
DarkChem Lite v0.1.0
[M+H]+171.69351
predicted
DeepCCS 1.0 (2019)
[M+Na]+222.3238928
predicted
DarkChem Lite v0.1.0
[M+Na]+225.8385928
predicted
DarkChem Lite v0.1.0
[M+Na]+206.1454928
predicted
DarkChem Lite v0.1.0
[M+Na]+230.3052928
predicted
DarkChem Lite v0.1.0
[M+Na]+179.74715
predicted
DeepCCS 1.0 (2019)

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transporter activity
Specific Function
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4...
Gene Name
ABCC6
Uniprot ID
O95255
Uniprot Name
Multidrug resistance-associated protein 6
Molecular Weight
164904.81 Da
References
  1. Ilias A, Urban Z, Seidl TL, Le Saux O, Sinko E, Boyd CD, Sarkadi B, Varadi A: Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). J Biol Chem. 2002 May 10;277(19):16860-7. Epub 2002 Mar 5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Sauna ZE, Peng XH, Nandigama K, Tekle S, Ambudkar SV: The molecular basis of the action of disulfiram as a modulator of the multidrug resistance-linked ATP binding cassette transporters MDR1 (ABCB1) and MRP1 (ABCC1). Mol Pharmacol. 2004 Mar;65(3):675-84. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
ATP as a substrate for hydrolysis by ABCC1
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Westlake CJ, Payen L, Gao M, Cole SP, Deeley RG: Identification and characterization of functionally important elements in the multidrug resistance protein 1 COOH-terminal region. J Biol Chem. 2004 Dec 17;279(51):53571-83. Epub 2004 Sep 30. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Cofactor
General Function
Pdz domain binding
Specific Function
Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO...
Gene Name
CFTR
Uniprot ID
P13569
Uniprot Name
Cystic fibrosis transmembrane conductance regulator
Molecular Weight
168139.895 Da
References
  1. Berger AL, Ikuma M, Welsh MJ: Normal gating of CFTR requires ATP binding to both nucleotide-binding domains and hydrolysis at the second nucleotide-binding domain. Proc Natl Acad Sci U S A. 2005 Jan 11;102(2):455-60. Epub 2004 Dec 27. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate...
Gene Name
PIK3CA
Uniprot ID
P42336
Uniprot Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Molecular Weight
124283.025 Da
References
  1. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ: The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-t hieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated ser...
Gene Name
CSNK2A1
Uniprot ID
P68400
Uniprot Name
Casein kinase II subunit alpha
Molecular Weight
45143.25 Da
References
  1. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM: Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transcription factor binding
Specific Function
Participates in Wnt signaling (By similarity). Plays a complex role in regulating the basal catalytic activity of the alpha subunit.
Gene Name
CSNK2B
Uniprot ID
P67870
Uniprot Name
Casein kinase II subunit beta
Molecular Weight
24942.25 Da
References
  1. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM: Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Receptor activity
Specific Function
Receptor for ATP and ADP coupled to G-proteins that activate both phosphatidylinositol-calcium and adenylyl cyclase second messenger systems. Not activated by UTP or UDP.
Gene Name
P2RY11
Uniprot ID
Q96G91
Uniprot Name
P2Y purinoceptor 11
Molecular Weight
40344.755 Da
References
  1. Xiao Z, Yang M, Lv Q, Wang W, Deng M, Liu X, He Q, Chen X, Chen M, Fang L, Xie X, Hu J: P2Y11 impairs cell proliferation by induction of cell cycle arrest and sensitizes endothelial cells to cisplatin-induced cell death. J Cell Biochem. 2011 Sep;112(9):2257-65. doi: 10.1002/jcb.23144. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Signal transducer activity
Specific Function
Serine/threonine-protein phosphatase that dephosphorylates a myriad of proteins involved in different signaling pathways including the kinases CSNK1E, ASK1/MAP3K5, PRKDC and RAF1, the nuclear recep...
Gene Name
PPP5C
Uniprot ID
P53041
Uniprot Name
Serine/threonine-protein phosphatase 5
Molecular Weight
56878.22 Da
References
  1. Hong TJ, Kim S, Wi AR, Lee P, Kang M, Jeong JH, Hahn JS: Dynamic nucleotide-dependent interactions of cysteine- and histidine-rich domain (CHORD)-containing Hsp90 cochaperones Chp-1 and melusin with cochaperones PP5 and Sgt1. J Biol Chem. 2013 Jan 4;288(1):215-22. doi: 10.1074/jbc.M112.398636. Epub 2012 Nov 26. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Receptor binding
Specific Function
Non-receptor tyrosine-protein kinase that plays an ABL1-overlapping role in key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, ce...
Gene Name
ABL2
Uniprot ID
P42684
Uniprot Name
Abelson tyrosine-protein kinase 2
Molecular Weight
128341.935 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Syntaxin binding
Specific Function
cAMP-dependent and sulfonylurea-sensitive anion transporter. Key gatekeeper influencing intracellular cholesterol transport.
Gene Name
ABCA1
Uniprot ID
O95477
Uniprot Name
ATP-binding cassette sub-family A member 1
Molecular Weight
254299.89 Da
References
  1. Porchay I, Pean F, Bellili N, Royer B, Cogneau J, Chesnier MC, Caradec A, Tichet J, Balkau B, Marre M, Fumeron F: ABCA1 single nucleotide polymorphisms on high-density lipoprotein-cholesterol and overweight: the D.E.S.I.R. study. Obesity (Silver Spring). 2006 Nov;14(11):1874-9. [Article]
  2. Badeau R, Jauhiainen M, Metso J, Nikander E, Tikkanen MJ, Ylikorkala O, Mikkola TS: Effect of isolated isoflavone supplementation on ABCA1-dependent cholesterol efflux potential in postmenopausal women. Menopause. 2007 Mar-Apr;14(2):293-9. [Article]
  3. Zarubica A, Trompier D, Chimini G: ABCA1, from pathology to membrane function. Pflugers Arch. 2007 Feb;453(5):569-79. Epub 2006 Jul 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Atp binding
Specific Function
Activates acetate so that it can be used for lipid synthesis or for energy generation.
Gene Name
ACSS2
Uniprot ID
Q9NR19
Uniprot Name
Acetyl-coenzyme A synthetase, cytoplasmic
Molecular Weight
78579.11 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Starai VJ, Celic I, Cole RN, Boeke JD, Escalante-Semerena JC: Sir2-dependent activation of acetyl-CoA synthetase by deacetylation of active lysine. Science. 2002 Dec 20;298(5602):2390-2. [Article]
  4. Schuler AJ, Jenkins D: Enhanced biological phosphorus removal from wastewater by biomass with different phosphorus contents, Part II: Anaerobic adenosine triphosphate utilization and acetate uptake rates. Water Environ Res. 2003 Nov-Dec;75(6):499-511. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Neuronal orphan receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis a...
Gene Name
ALK
Uniprot ID
Q9UM73
Uniprot Name
ALK tyrosine kinase receptor
Molecular Weight
176440.535 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Regulatory subunit of the dimeric UBA3-NAE1 E1 enzyme. E1 activates NEDD8 by first adenylating its C-terminal glycine residue with ATP, thereafter linking this residue to the side chain of the cata...
Gene Name
NAE1
Uniprot ID
Q13564
Uniprot Name
NEDD8-activating enzyme E1 regulatory subunit
Molecular Weight
60245.795 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Tau-protein kinase activity
Specific Function
Catalytic subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular A...
Gene Name
PRKAA1
Uniprot ID
Q13131
Uniprot Name
5'-AMP-activated protein kinase catalytic subunit alpha-1
Molecular Weight
64008.64 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Receptor signaling protein activity
Specific Function
Involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May also regulate the TOR signaling cascade.Isoform 2: Serves as a positive regulator of myogenic differenti...
Gene Name
ARAF
Uniprot ID
P10398
Uniprot Name
Serine/threonine-protein kinase A-Raf
Molecular Weight
67584.825 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transmembrane receptor protein serine/threonine kinase activity
Specific Function
Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. On ligand binding, forms a receptor complex consisting of two type II and...
Gene Name
ACVRL1
Uniprot ID
P37023
Uniprot Name
Serine/threonine-protein kinase receptor R3
Molecular Weight
56124.03 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Long-chain fatty acid-coa ligase activity
Specific Function
Activation of long-chain fatty acids for both synthesis of cellular lipids, and degradation via beta-oxidation. Preferentially uses palmitoleate, oleate and linoleate.
Gene Name
ACSL1
Uniprot ID
P33121
Uniprot Name
Long-chain-fatty-acid--CoA ligase 1
Molecular Weight
77942.685 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Nucleotide binding
Specific Function
May have a critical role in the maintenance of a constant composition of intracellular purine/pyrimidine nucleotides in cooperation with other nucleotidases. Preferentially hydrolyzes inosine 5'-mo...
Gene Name
NT5C2
Uniprot ID
P49902
Uniprot Name
Cytosolic purine 5'-nucleotidase
Molecular Weight
64969.2 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transporter activity
Specific Function
ATPase required for the post-translational delivery of tail-anchored (TA) proteins to the endoplasmic reticulum. Recognizes and selectively binds the transmembrane domain of TA proteins in the cyto...
Gene Name
ASNA1
Uniprot ID
O43681
Uniprot Name
ATPase ASNA1
Molecular Weight
38792.445 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transporter activity
Specific Function
Subunit of ATP-sensitive potassium channels (KATP). Can form cardiac and smooth muscle-type KATP channels with KCNJ11. KCNJ11 forms the channel pore while ABCC9 is required for activation and regul...
Gene Name
ABCC9
Uniprot ID
O60706
Uniprot Name
ATP-binding cassette sub-family C member 9
Molecular Weight
174221.7 Da
References
  1. Zhao JL, Yang YJ, You SJ, Jing ZC, Wu YJ, Cheng JL, Gao RL: Pretreatment with fosinopril or valsartan reduces myocardial no-reflow after acute myocardial infarction and reperfusion. Coron Artery Dis. 2006 Aug;17(5):463-9. [Article]
  2. Yang YJ, Zhao JL, You SJ, Wu YJ, Jing ZC, Gao RL, Chen ZJ: Post-infarction treatment with simvastatin reduces myocardial no-reflow by opening of the KATP channel. Eur J Heart Fail. 2007 Jan;9(1):30-6. Epub 2006 Jul 7. [Article]
  3. Bryan J, Munoz A, Zhang X, Dufer M, Drews G, Krippeit-Drews P, Aguilar-Bryan L: ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18. Epub 2006 Aug 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein serine/threonine/tyrosine kinase activity
Specific Function
AKT1 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, ...
Gene Name
AKT1
Uniprot ID
P31749
Uniprot Name
RAC-alpha serine/threonine-protein kinase
Molecular Weight
55686.035 Da
References
  1. Van Meter TE, Broaddus WC, Cash D, Fillmore H: Cotreatment with a novel phosphoinositide analogue inhibitor and carmustine enhances chemotherapeutic efficacy by attenuating AKT activity in gliomas. Cancer. 2006 Nov 15;107(10):2446-54. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein kinase activity
Specific Function
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes w...
Gene Name
ADRBK1
Uniprot ID
P25098
Uniprot Name
Beta-adrenergic receptor kinase 1
Molecular Weight
79572.96 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Nucleotide binding
Specific Function
Oligomeric Apaf-1 mediates the cytochrome c-dependent autocatalytic activation of pro-caspase-9 (Apaf-3), leading to the activation of caspase-3 and apoptosis. This activation requires ATP. Isoform...
Gene Name
APAF1
Uniprot ID
O14727
Uniprot Name
Apoptotic protease-activating factor 1
Molecular Weight
141838.815 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Chinnaiyan AM: The apoptosome: heart and soul of the cell death machine. Neoplasia. 1999 Apr;1(1):5-15. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Atp binding
Specific Function
Important for maintaining normal body temperature during fasting and for energy homeostasis. Essential for energy expenditure under ketogenic conditions (By similarity). Converts acetate to acetyl-...
Gene Name
ACSS1
Uniprot ID
Q9NUB1
Uniprot Name
Acetyl-coenzyme A synthetase 2-like, mitochondrial
Molecular Weight
74856.1 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Transmembrane serine/threonine kinase activin type-1 receptor forming an activin receptor complex with activin receptor type-2 (ACVR2A or ACVR2B). Transduces the activin signal from the cell surfac...
Gene Name
ACVR1B
Uniprot ID
P36896
Uniprot Name
Activin receptor type-1B
Molecular Weight
56806.05 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transmembrane receptor protein serine/threonine kinase activity
Specific Function
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which auto...
Gene Name
ACVR1
Uniprot ID
Q04771
Uniprot Name
Activin receptor type-1
Molecular Weight
57152.41 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Snow KL, Moseley RH: Effect of thiazolidinediones on bile acid transport in rat liver. Life Sci. 2007 Jan 30;80(8):732-40. Epub 2006 Nov 10. [Article]
  2. Suchy FJ, Ananthanarayanan M: Bile salt excretory pump: biology and pathobiology. J Pediatr Gastroenterol Nutr. 2006 Jul;43 Suppl 1:S10-6. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein homodimerization activity
Specific Function
Not Available
Gene Name
ASNS
Uniprot ID
P08243
Uniprot Name
Asparagine synthetase [glutamine-hydrolyzing]
Molecular Weight
64369.39 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Serine/threonine-protein kinase that acts like an antiapoptotic protein that counters TRAIL/TNFSF10-induced apoptosis by inducing phosphorylation of BIRC5 at 'Thr-34'.
Gene Name
CDK15
Uniprot ID
Q96Q40
Uniprot Name
Cyclin-dependent kinase 15
Molecular Weight
49022.64 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Adenine transmembrane transporter activity
Specific Function
Catalyzes the exchange of cytoplasmic ADP with mitochondrial ATP across the mitochondrial inner membrane.
Gene Name
SLC25A4
Uniprot ID
P12235
Uniprot Name
ADP/ATP translocase 1
Molecular Weight
33064.265 Da
References
  1. Walther T, Tschope C, Sterner-Kock A, Westermann D, Heringer-Walther S, Riad A, Nikolic A, Wang Y, Ebermann L, Siems WE, Bader M, Shakibaei M, Schultheiss HP, Dorner A: Accelerated mitochondrial adenosine diphosphate/adenosine triphosphate transport improves hypertension-induced heart disease. Circulation. 2007 Jan 23;115(3):333-44. Epub 2007 Jan 8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Sulfonylurea receptor activity
Specific Function
Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
Gene Name
ABCC8
Uniprot ID
Q09428
Uniprot Name
ATP-binding cassette sub-family C member 8
Molecular Weight
176990.36 Da
References
  1. Nakamura A, Kawahito S, Kawano T, Nazari H, Takahashi A, Kitahata H, Nakaya Y, Oshita S: Differential effects of etomidate and midazolam on vascular adenosine triphosphate-sensitive potassium channels: isometric tension and patch clamp studies. Anesthesiology. 2007 Mar;106(3):515-22. [Article]
  2. Bienengraeber M, Warltier DC, Bosnjak ZJ, Stadnicka A: Mechanism of cardiac sarcolemmal adenosine triphosphate-sensitive potassium channel activation by isoflurane in a heterologous expression system. Anesthesiology. 2006 Sep;105(3):534-40. [Article]
  3. Bryan J, Munoz A, Zhang X, Dufer M, Drews G, Krippeit-Drews P, Aguilar-Bryan L: ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18. Epub 2006 Aug 8. [Article]
  4. Tanaka K, Kawano T, Nakamura A, Nazari H, Kawahito S, Oshita S, Takahashi A, Nakaya Y: Isoflurane activates sarcolemmal adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells: a role for protein kinase A. Anesthesiology. 2007 May;106(5):984-91. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific Function
Is indirectly involved in the control of blood pressure.
Gene Name
ASS1
Uniprot ID
P00966
Uniprot Name
Argininosuccinate synthase
Molecular Weight
46530.055 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
ATP-dependent protease which is essential for axonal development.
Gene Name
AFG3L2
Uniprot ID
Q9Y4W6
Uniprot Name
AFG3-like protein 2
Molecular Weight
88583.03 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein kinase activity
Specific Function
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
Gene Name
ADRBK2
Uniprot ID
P35626
Uniprot Name
Beta-adrenergic receptor kinase 2
Molecular Weight
79709.085 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transforming growth factor beta receptor activity, type ii
Specific Function
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which auto...
Gene Name
AMHR2
Uniprot ID
Q16671
Uniprot Name
Anti-Muellerian hormone type-2 receptor
Molecular Weight
62749.02 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ww domain binding
Specific Function
Non-receptor tyrosine-protein and serine/threonine-protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals ...
Gene Name
TNK2
Uniprot ID
Q07912
Uniprot Name
Activated CDC42 kinase 1
Molecular Weight
114567.605 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Syntaxin binding
Specific Function
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility a...
Gene Name
ABL1
Uniprot ID
P00519
Uniprot Name
Tyrosine-protein kinase ABL1
Molecular Weight
122871.435 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Metal ion binding
Specific Function
Catalyzes the formation of the signaling molecule cAMP in response to G-protein signaling. Mediates responses to increased cellular Ca(2+)/calmodulin levels (By similarity). May be involved in regu...
Gene Name
ADCY1
Uniprot ID
Q08828
Uniprot Name
Adenylate cyclase type 1
Molecular Weight
123438.85 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Lage H: MDR1/P-glycoprotein (ABCB1) as target for RNA interference-mediated reversal of multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):813-21. [Article]
  2. Gardner ER, Burger H, van Schaik RH, van Oosterom AT, de Bruijn EA, Guetens G, Prenen H, de Jong FA, Baker SD, Bates SE, Figg WD, Verweij J, Sparreboom A, Nooter K: Association of enzyme and transporter genotypes with the pharmacokinetics of imatinib. Clin Pharmacol Ther. 2006 Aug;80(2):192-201. [Article]
  3. Blume H, Donath F, Warnke A, Schug BS: Pharmacokinetic drug interaction profiles of proton pump inhibitors. Drug Saf. 2006;29(9):769-84. doi: 10.2165/00002018-200629090-00002. [Article]
  4. Gervasini G, Carrillo JA, Garcia M, San Jose C, Cabanillas A, Benitez J: Adenosine triphosphate-binding cassette B1 (ABCB1) (multidrug resistance 1) G2677T/A gene polymorphism is associated with high risk of lung cancer. Cancer. 2006 Dec 15;107(12):2850-7. [Article]
  5. Fukui N, Suzuki Y, Sawamura K, Sugai T, Watanabe J, Inoue Y, Someya T: Dose-dependent effects of the 3435 C>T genotype of ABCB1 gene on the steady-state plasma concentration of fluvoxamine in psychiatric patients. Ther Drug Monit. 2007 Apr;29(2):185-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Toxin transporter activity
Specific Function
Transporter involved in macrophage lipid homeostasis. Is an active component of the macrophage lipid export complex. Could also be involved in intracellular lipid transport processes. The role in c...
Gene Name
ABCG1
Uniprot ID
P45844
Uniprot Name
ATP-binding cassette sub-family G member 1
Molecular Weight
75591.275 Da
References
  1. Lage H: MDR1/P-glycoprotein (ABCB1) as target for RNA interference-mediated reversal of multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):813-21. [Article]
  2. Materna V, Stege A, Surowiak P, Priebsch A, Lage H: RNA interference-triggered reversal of ABCC2-dependent cisplatin resistance in human cancer cells. Biochem Biophys Res Commun. 2006 Sep 15;348(1):153-7. Epub 2006 Jul 14. [Article]
  3. Thomas AC, Cullup T, Norgett EE, Hill T, Barton S, Dale BA, Sprecher E, Sheridan E, Taylor AE, Wilroy RS, DeLozier C, Burrows N, Goodyear H, Fleckman P, Stephens KG, Mehta L, Watson RM, Graham R, Wolf R, Slavotinek A, Martin M, Bourn D, Mein CA, O'Toole EA, Kelsell DP: ABCA12 is the major harlequin ichthyosis gene. J Invest Dermatol. 2006 Nov;126(11):2408-13. Epub 2006 Aug 10. [Article]
  4. Girardin F: Membrane transporter proteins: a challenge for CNS drug development. Dialogues Clin Neurosci. 2006;8(3):311-21. [Article]
  5. Pinkett HW, Lee AT, Lum P, Locher KP, Rees DC: An inward-facing conformation of a putative metal-chelate-type ABC transporter. Science. 2007 Jan 19;315(5810):373-7. Epub 2006 Dec 7. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Materna V, Stege A, Surowiak P, Priebsch A, Lage H: RNA interference-triggered reversal of ABCC2-dependent cisplatin resistance in human cancer cells. Biochem Biophys Res Commun. 2006 Sep 15;348(1):153-7. Epub 2006 Jul 14. [Article]
  2. Rau T, Erney B, Gores R, Eschenhagen T, Beck J, Langer T: High-dose methotrexate in pediatric acute lymphoblastic leukemia: impact of ABCC2 polymorphisms on plasma concentrations. Clin Pharmacol Ther. 2006 Nov;80(5):468-76. [Article]
  3. Li GX, Pei QL, Gao Y, Liu KM, Nie JS, Han G, Qiu YL, Zhang WP: Protective effects of hepatocellular canalicular conjugate export pump (Mrp2) on sodium arsenite-induced hepatic dysfunction in rats. Exp Toxicol Pathol. 2007 Aug;58(6):447-53. Epub 2007 Apr 30. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Poly(a) rna binding
Specific Function
ATP dependent phosphorylation of adenosine and other related nucleoside analogs to monophosphate derivatives. Serves as a potential regulator of concentrations of extracellular adenosine and intrac...
Gene Name
ADK
Uniprot ID
P55263
Uniprot Name
Adenosine kinase
Molecular Weight
40545.075 Da
References
  1. Park J, Gupta RS: Adenosine kinase and ribokinase--the RK family of proteins. Cell Mol Life Sci. 2008 Sep;65(18):2875-96. doi: 10.1007/s00018-008-8123-1. [Article]
  2. Leoncini R, Vannoni D, Santoro A, Giglioni S, Carli R, Marinello E: Adenosine kinase from rat liver: new biochemical properties. Nucleosides Nucleotides Nucleic Acids. 2006;25(9-11):1107-12. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 19:36