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Showing drug card for Norethindrone (DB00717)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:04:30
Primary Accession Number DB00717
Secondary Accession Number
  • APRD00679
Name Norethindrone
Drug Type
  • Approved
  • Small Molecule
Description A synthetic progestational hormone with actions similar to those of progesterone but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception. [PubChem]
Synonyms Not Available
Brand Names
  1. Anhydrohydroxynorprogesterone
  2. Anovulatorio
  3. Anovule
  4. Aygestin
  5. Binovum
  6. Brevicon
  7. Brevinor
  8. Brevinor 21
  9. Brevinor 28
  10. Brevinor-1 21
  11. Brevinor-1 28
  12. Camila
  13. Ciclovulan
  14. Conceplan
  15. Conludaf
  16. Conludag
  17. Demulen
  18. ENT
  19. Errin
  20. Estrinor
  21. Ethinylnortestosterone
  22. Ethynylmortestosterone
  23. Ethynylnortestosterone
  24. Gencept
  25. Genora
  26. Gestest
  27. Jenest
  28. Jenest-28
  29. Loestrin
  30. Menzol
  31. Microneth
  32. Micronett
  33. Micronor
  34. Micronovum
  35. Milli
  36. Mini-Pe
  37. Mini-Pill
  38. Minovlar
  39. Modicon
  40. N.E.E.
  41. NET
  42. Necon
  43. Nelova
  44. Neocon
  45. Nodiol
  46. Nor-Q.D.
  47. Nor-Qd
  48. Noraethisteronum
  49. Noralutin
  50. Norcept
  51. Norcept-E
  52. Norcolut
  53. Noresthisterone
  54. Norethadrone
  55. Norethin
  56. Norethin 1/35 E
  57. Norethin 1/50 M
  58. Norethindrone Acetate
  59. Norethindrone Norethisterone
  60. Norethisteron
  61. Norethisterone
  62. Norethisterone [Progestins]
  63. Norethisteronum [INN-Latin]
  64. Norethyndron
  65. Norethynodron
  66. Norethynodrone
  67. Noretisterona [INN-Spanish]
  68. Noretisterone [Dcit]
  69. Norfor
  70. Norgestin
  71. Noriday
  72. Noriday 28
  73. Norimin
  74. Norinyl
  75. Norlestrin
  76. Norlutate
  77. Norluten
  78. Norlutin
  79. Norluton
  80. Normapause
  81. Norpregneninlone
  82. Norpregneninolone
  83. Norpregneninotone
  84. Orlest
  85. Ortho 1 35
  86. Ortho 7 7 7
  87. Ortho-Novum
  88. Ortho-Novum 1 35
  89. Ortho-Novum 1 50
  90. Ortho-Novum 7 7 7
  91. Ovcon
  92. Ovysmen
  93. Ovysmen 0.5 35
  94. Ovysmen 1 35
  95. Palonyl
  96. Perovex
  97. Primolut N
  98. Primolut-N
  99. Proluteasi
  100. Synphase
  101. Synphasic 28
  102. Tri-Norinyl
  103. Triella
  104. Trinovum
  105. Trinovum 21
  106. Utovlan
  107. Utovlar
Brand Mixtures
  1. Brevicon 0.5/35 21 Tab (Ethinyl Estradiol + Norethindrone)
  2. Brevicon 0.5/35 28 Tab (Ethinyl Estradiol + Norethindrone)
  3. Brevicon 0.5/35 Tablets (21-Day Pack) (Ethinyl Estradiol + Norethindrone)
  4. Brevicon 0.5/35 Tablets (28-Day Pack) (Ethinyl Estradiol + Norethindrone)
  5. Brevicon 1/35 21 Tab (Ethinyl Estradiol + Norethindrone)
  6. Brevicon 1/35 28 Tab (Ethinyl Estradiol + Norethindrone)
  7. Brevicon 1/35 Tablets (21-Day Pack) (Ethinyl Estradiol + Norethindrone)
  8. Brevicon 1/35 Tablets (28-Day Pack) (Ethinyl Estradiol + Norethindrone)
  9. Estalis 140/50 Mcg (Estradiol + Norethindrone Acetate)
  10. Estalis 250/50 Mcg (Estradiol + Norethindrone Acetate)
  11. Estalis Sequi (Estradiol + Norethindrone Acetate)
  12. Estracomb (Estradiol + Norethindrone Acetate)
  13. Femhrt 1/5 (Ethinyl Estradiol + Norethindrone Acetate)
  14. Loestrin 1.5/30 21day Pak (Ethinyl Estradiol + Norethindrone Acetate)
  15. Loestrin 1.5/30 28day Pack (Ethinyl Estradiol + Norethindrone Acetate)
  16. Minestrin 1/20 21 (Ethinyl Estradiol + Norethindrone Acetate)
  17. Minestrin 1/20 28 (Ethinyl Estradiol + Norethindrone Acetate)
  18. Norinyl 1/50 - (21-Day Regimen) (Mestranol + Norethindrone)
  19. Norinyl 1/50 - (28-Day Regimen) (Mestranol + Norethindrone)
  20. Norinyl 1/50 21 Tab (Mestranol + Norethindrone)
  21. Norinyl 1/50 28 Tab (Mestranol + Norethindrone)
  22. Ortho 0.5/35 Tablets (21 Day) (Ethinyl Estradiol + Norethindrone)
  23. Ortho 0.5/35 Tablets (28day) (Ethinyl Estradiol + Norethindrone)
  24. Ortho 1/35 Tablets (21 Day) (Ethinyl Estradiol + Norethindrone)
  25. Ortho 1/35 Tablets (28 Day) (Ethinyl Estradiol + Norethindrone)
  26. Ortho 10/11 Tablets (21 Day) (Ethinyl Estradiol + Norethindrone)
  27. Ortho 10/11 Tablets (28 Day) (Ethinyl Estradiol + Norethindrone)
  28. Ortho 7/7/7 Tablets (21 Day) (Ethinyl Estradiol + Norethindrone)
  29. Ortho 7/7/7 Tablets (28 Day) (Ethinyl Estradiol + Norethindrone)
  30. Ortho-Novum 1/50 Tablets (21 Day) (Mestranol + Norethindrone)
  31. Ortho-Novum 1/50 Tablets (28 Day) (Mestranol + Norethindrone)
  32. Select 1/35 (21-Day) (Ethinyl Estradiol + Norethindrone)
  33. Select 1/35 (28-Day) (Ethinyl Estradiol + Norethindrone)
  34. Synphasic 21 Tablets (Ethinyl Estradiol + Norethindrone)
  35. Synphasic 28 Tablets (Ethinyl Estradiol + Norethindrone)
  36. Synphasic-28 Tablets (Ethinyl Estradiol + Norethindrone)
Chemical IUPAC Name (8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
Chemical Formula C20H26O2
Chemical Structure Structure
CAS Registry Number 68-22-4
InChI Identifier InChI=1/C20H26O2/c1-3-20(22)11-9-18-17-6-4-13-12-14(21)5-7-15(13)16(17)8-10-19(18,20)2/h1,12,15-18,22H,4-11H2,2H3/t15-,16+,17+,18-,19-,20-/m0/s1
InChI Key VIKNJXKGJWUCNN-XGXHKTLJBN
KEGG Drug D00182 Link Image
KEGG Compound C05028 Link Image
PubChem Compound 6230 Link Image
PubChem Substance 7847250 Link Image
ChEBI ID Not Available
PharmGKB ID PA450651 Link Image
HET ID NDR Link Image
GenBank ID Not Available
Drug ID Number [DIN] 00023760 Link Image
RxList Link http://www.rxlist.com/cgi/generic2/norethin.htm Link Image
PDRhealth Link http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ayg1666.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Norethindrone Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Djerassi et al., J. Am. Chem. Soc. 76, 4092(1954)
Average Molecular Weight 298.4192
Monoisotopic Molecular Weight 298.1933
State Solid
Melting Point 203.5 oC
Experimental Water Solubility 7.04 mg/L Source: PhysProp
Predicted Water Solubility 6.68e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3.2 Source: PhysProp
Predicted LogP 2.72 Calculated using ALOGPS
Experimental LogS -4.57 [ADME Research, USCD]
Predicted LogS -4.65 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@H]34)[C@@H]1CC[C@@]2(O)C#C
Canonical SMILES CC12CCC3C(CCC4=CC(=O)CCC34)C1CCC2(O)C#C
Drug Category
  • Contraceptives, Oral, Synthetic
  • Progestins
ATC Codes
AHFS Codes
  • 68:12.00
Indication For use as an oral contraceptive in the prevention of pregnancy.
Pharmacology Norethindrone is a synthetic oral progestin. It is used for contraception or to treat such conditions as secondary amenorrhea, abnormal uterine bleeding, and endometriosis. As an oral contraceptive, norethindrone is available as either a single agent or in combination with an estrogen.
Mechanism of Action Progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
Absorption Absolute oral bioavailability approximately 64%
Toxicity Not Available
Protein Binding >95%
Biotransformation Hepatic
Half Life 7 hours
Dosage Forms
Form Route
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Acitretin Acitretine may cause a loss of contraceptive effect
Amobarbital This product may cause a slight decrease of contraceptive effect
Aprobarbital This product may cause a slight decrease of contraceptive effect
Bosentan Bosentan decreases the effect of the contraceptive
Butabarbital This product may cause a slight decrease of contraceptive effect
Butalbital This product may cause a slight decrease of contraceptive effect
Butethal This product may cause a slight decrease of contraceptive effect
Carbamazepine This product may cause a slight decrease of contraceptive effect
Ethotoin This product may cause a slight decrease of contraceptive effect
Fosphenytoin This product may cause a slight decrease of contraceptive effect
Griseofulvin This product may cause a slight decrease of contraceptive effect
Heptabarbital This product may cause a slight decrease of contraceptive effect
Hexobarbital This product may cause a slight decrease of contraceptive effect
Lamotrigine The oral contraceptive decreases the effect of lamotrigine
Mephenytoin This product may cause a slight decrease of contraceptive effect
Methohexital This product may cause a slight decrease of contraceptive effect
Methylphenobarbital This product may cause a slight decrease of contraceptive effect
Pentobarbital This product may cause a slight decrease of contraceptive effect
Phenobarbital This product may cause a slight decrease of contraceptive effect
Phenytoin This product may cause a slight decrease of contraceptive effect
Pioglitazone Possible loss of contraceptive effect
Primidone This product may cause a slight decrease of contraceptive effect
Rifabutin This product may cause a slight decrease of contraceptive effect
Rifampin This product may cause a slight decrease of contraceptive effect
Rifapentine This product may cause a slight decrease of contraceptive effect
Secobarbital This product may cause a slight decrease of contraceptive effect
St. John's Wort St. John's Wort could reduce the contraceptive effect
Talbutal This product may cause a slight decrease of contraceptive effect
Tizanidine The contraceptive increases the effect of tizanidine
Troglitazone Possible loss of contraceptive effect
Food Interactions
  • Take without regard to meals.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
  4. PDRhealth Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
Targets
  1. Progesterone receptor
  2. Sex hormone-binding globulin
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Drug Target 1 [top]
Target 1 ID 614
Target 1 Name Progesterone receptor
Target 1 Synonyms
  1. PR
Target 1 Gene Name PGR
Target 1 Protein Sequence >Progesterone receptor 
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA
PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA
AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK
PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV
MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD
CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG
PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC
KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP
YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN
YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV
GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ
LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP
DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ
FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA
LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
Target 1 Number of Residues 948
Target 1 Molecular Weight 98982
Target 1 Theoretical pI 6.45
Target 1 GO Classification
Function
steroid binding
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 1 General Function Involved in transcription factor activity
Target 1 Specific Function The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 35652 Link Image
Target 1 UniProtKB/Swiss-Prot ID P06401 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name PRGR_HUMAN Link Image
Target 1 PDB ID 1SQN Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Nucleus
Target 1 Gene Sequence >2802 bp 
ATGACTGAGCTGAAGGCAAAGGGTCCCCGGGCTCCCCACGTGGCGGGCGGCCCGCCCTCC
CCCGAGGTCGGATCCCCACTGCTGTGTCGCCCAGCCGCAGGTCCGTTCCCGGGGAGCCAG
ACCTCGGACACCTTGCCTGAAGTTTCGGCCATACCTATCTCCCTGGACGGGCTACTCTTC
CCTCGGCCCTGCCAGGGACAGGACCCCTCCGACGAAAAGACGCAGGACCAGCAGTCGCTG
TCGGACGTGGAGGGCGCATATTCCAGAGCTGAAGCTACAAGGGGTGCTGGAGGCAGCAGT
TCTAGTCCCCCAGAAAAGGACAGCGGACTGCTGGACAGTGTCTTGGACACTCTGTTGGCG
CCCTCAGGTCCCGGGCAGAGCCAACCCAGCCCTCCCGCCTGCGAGGTCACCAGCTCTTGG
TGCCTGTTTGGCCCCGAACTTCCCGAAGATCCACCGGCTGCCCCCGCCACCCAGCGGGTG
TTGTCCCCGCTCATGAGCCGGTCCGGGTGCAAGGTTGGAGACAGCTCCGGGACGGCAGCT
GCCCATAAAGTGCTGCCCCGGGGCCTGTCACCAGCCCGGCAGCTGCTGCTCCCGGCCTCT
GAGAGCCCTCACTGGTCCGGGGCCCCAGTGAAGCCGTCTCCGCAGGCCGCTGCGGTGGAG
GTTGAGGAGGAGGATAGCTCTGAGTCCGAGGAGTCTGCGGGTCCGCTTCTGAAGGGCAAA
CCTCGGGCTCTGGGTGGCGCGGCGGCTGGAGGAGGAGCCGCGGCTTGTCCGCCGGGGGCG
GCAGCAGGAGGCGTCGCCCTGGTCCCCAAGGAAGATTCCCGCTTCTCAGCGCCCAGGGTC
GCCCTGGTGGAGCAGGACGCGCCGATGGCGCCCGGGCGCTCCCCGCTGGCCACCACGGTG
ATGGATTTCATCCACGTGCCTATCCTGCCTCTCAATCACGCCTTATTGGCAGCCCGCACT
CGGCAGCTGCTGGAAGACGAAAGTTACGACGGCGGGGCCGGGGCTGCCAGCGCCTTTGCC
CCGCCGCGGACTTCACCCTGTGCCTCGTCCACCCCGGTCGCTGTAGGCGACTTCCCCGAC
TGCGCGTACCCGCCCGACGCCGAGCCCAAGGACGACGCGTACCCTCTCTATAGCGACTTC
CAGCCGCCCGCTCTAAAGATAAAGGAGGAGGAGGAAGGCGCGGAGGCCTCCGCGCGCTCC
CCGCGTTCCTACCTTGTGGCCGGTGCCAACCCCGCAGCCTTCCCGGATTTCCCGTTGGGG
CCACCGCCCCCGCTGCCGCCGCGAGCGACCCCATCCAGACCCGGGGAAGCGGCGGTGACG
GCCGCACCCGCCAGTGCCTCAGTCTCGTCTGCGTCCTCCTCGGGGTCGACCCTGGAGTGC
ATCCTGTACAAAGCGGAGGGCGCGCCGCCCCAGCAGGGCCCGTTCGCGCCGCCGCCCTGC
AAGGCGCCGGGCGCGAGCGGCTGCCTGCTCCCGCGGGACGGCCTGCCCTCCACCTCCGCC
TCTGCCGCCGCCGCCGGGGCGGCCCCCGCGCTCTACCCTGCACTCGGCCTCAACGGGCTC
CCGCAGCTCGGCTACCAGGCCGCCGTGCTCAAGGAGGGCCTGCCGCAGGTCTACCCGCCC
TATCTCAACTACCTGAGGCCGGATTCAGAAGCCAGCCAGAGCCCACAATACAGCTTCGAG
TCATTACCTCAGAAGATTTGTTTAATCTGTGGGGATGAAGCATCAGGCTGTCATTATGGT
GTCCTTACCTGTGGGAGCTGTAAGGTCTTCTTTAAGAGGGCAATGGAAGGGCAGCACAAC
TACTTATGTGCTGGAAGAAATGACTGCATCGTTGATAAAATCCGCAGAAAAAACTGCCCA
GCATGTCGCCTTAGAAAGTGCTGTCAGGCTGGCATGGTCCTTGGAGGTCGAAAATTTAAA
AAGTTCAATAAAGTCAGAGTTGTGAGAGCACTGGATGCTGTTGCTCTCCCACAGCCATTG
GGCGTTCCAAATGAAAGCCAAGCCCTAAGCCAGAGATTCACTTTTTCACCAGGTCAAGAC
ATACAGTTGATTCCACCACTGATCAACCTGTTAATGAGCATTGAACCAGATGTGATCTAT
GCAGGACATGACAACACAAAACCTGACACCTCCAGTTCTTTGCTGACAAGTCTTAATCAA
CTAGGCGAGAGGCAACTTCTTTCAGTAGTCAAGTGGTCTAAATCATTGCCAGGTTTTCGA
AACTTACATATTGATGACCAGATAACTCTCATTCAGTATTCTTGGATGAGCTTAATGGTG
TTTGGTCTAGGATGGAGATCCTACAAACATGTCAGTGGGCAGATGCTGTATTTTGCACCT
GATCTAATACTAAATGAACAGCGGATGAAAGAATCATCATTCTATTCATTATGCCTTACC
ATGTGGCAGATCCCACAGGAGTTTGTCAAGCTTCAAGTTAGCCAAGAAGAGTTCCTCTGT
ATGAAAGTATTGTTACTTCTTAATACAATTCCTTTGGAAGGGCTACGAAGTCAAACCCAG
TTTGAGGAGATGAGGTCAAGCTACATTAGAGAGCTCATCAAGGCAATTGGTTTGAGGCAA
AAAGGAGTTGTGTCGAGCTCACAGCGTTTCTATCAACTTACAAAACTTCTTGATAACTTG
CATGATCTTGTCAAACAGCTTCATCTGTACTGCTTGAATACATTTATCCAGTCCCGGGCA
CTGAGTGTTGAATTTCCAGAAATGATGTCTGAAGTTATTGCTGCACAATTACCCAAGATA
TTGGCAGGGATGGTGAAACCCCTTCTCTTTCATAAAAAGTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID PGR Link Image
Target 1 GenAtlas ID PGR Link Image
Target 1 HGNC ID HGNC:8910 Link Image
Target 1 Chromosome Location 11
Target 1 Locus 11q22-q23
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Knotts TA, Orkiszewski RS, Cook RG, Edwards DP, Weigel NL: Identification of a phosphorylation site in the hinge region of the human progesterone receptor and additional amino-terminal phosphorylation sites. J Biol Chem. 2001 Mar 16;276(11):8475-83. Epub 2000 Dec 7. [PubMed Link Image]
  2. Kastner P, Krust A, Turcotte B, Stropp U, Tora L, Gronemeyer H, Chambon P: Two distinct estrogen-regulated promoters generate transcripts encoding the two functionally different human progesterone receptor forms A and B. EMBO J. 1990 May;9(5):1603-14. [PubMed Link Image]
  3. Misrahi M, Atger M, d'Auriol L, Loosfelt H, Meriel C, Fridlansky F, Guiochon-Mantel A, Galibert F, Milgrom E: Complete amino acid sequence of the human progesterone receptor deduced from cloned cDNA. Biochem Biophys Res Commun. 1987 Mar 13;143(2):740-8. [PubMed Link Image]
  4. Williams SP, Sigler PB: Atomic structure of progesterone complexed with its receptor. Nature. 1998 May 28;393(6683):392-6. [PubMed Link Image]
Target 1 Drug References
  1. Mendoza-Rodriguez CA, Camacho-Arroyo I, Garcia GA, Cerbon MA: Variations of progesterone receptor and c-fos gene expression in the rat uterus after treatment with norethisterone and its A-ring reduced metabolites. Contraception. 1999 May;59(5):339-43. [PubMed Link Image]
  2. Madauss KP, Deng SJ, Austin RJ, Lambert MH, McLay I, Pritchard J, Short SA, Stewart EL, Uings IJ, Williams SP: Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. [PubMed Link Image]
  3. Garcia-Becerra R, Cooney AJ, Borja-Cacho E, Lemus AE, Perez-Palacios G, Larrea F: Comparative evaluation of androgen and progesterone receptor transcription selectivity indices of 19-nortestosterone-derived progestins. J Steroid Biochem Mol Biol. 2004 Jun;91(1-2):21-7. [PubMed Link Image]
  4. Mirkin S, Wong BC, Archer DF: Effect of 17 beta-estradiol, progesterone, synthetic progestins, tibolone, and tibolone metabolites on vascular endothelial growth factor mRNA in breast cancer cells. Fertil Steril. 2005 Aug;84(2):485-91. [PubMed Link Image]
  5. Pasapera AM, Cerbon MA, Castro I, Gutierrez R, Camacho-Arroyo I, Garcia GA, Perez-Palacios G: Norethisterone metabolites modulate the uteroglobin and progesterone receptor gene expression in prepubertal rabbits. Biol Reprod. 1995 Feb;52(2):426-32. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 756
Target 2 Name Sex hormone-binding globulin
Target 2 Synonyms
  1. ABP
  2. SBP
  3. SHBG
  4. Sex hormone-binding globulin precursor
  5. Sex steroid-binding protein
  6. TeBG
  7. Testis-specific androgen-binding protein
  8. Testosterone-estradiol- binding globulin
  9. Testosterone-estrogen-binding globulin
Target 2 Gene Name SHBG
Target 2 Protein Sequence >Sex hormone-binding globulin precursor 
MESRGPLATSRLLLLLLLLLLRHTRQGWALRPVLPTQSAHDPPAVHLSNGPGQEPIAVMT
FDLTKITKTSSSFEVRTWDPEGVIFYGDTNPKDDWFMLGLRDGRPEIQLHNHWAQLTVGA
GPRLDDGRWHQVEVKMEGDSVLLEVDGEEVLRLRQVSGPLTSKRHPIMRIALGGLLFPAS
NLRLPLVPALDGCLRRDSWLDKQAEISASAPTSLRSCDVESNPGIFLPPGTQAEFNLRDI
PQPHAEPWAFSLDLGLKQAAGSGHLLALGTPENPSWLSLHLQDQKVVLSSGSGPGLDLPL
VLGLPLQLKLSMSRVVLSQGSKMKALALPPLGLAPLLNLWAKPQGRLFLGALPGEDSSTS
FCLNGLWAQGQRLDVDQALNRSHEIWTHSCPQSPGNGTDASH
Target 2 Number of Residues 408
Target 2 Molecular Weight 43780
Target 2 Theoretical pI 6.70
Target 2 GO Classification Not Available
Target 2 General Function Involved in androgen binding
Target 2 Specific Function Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone, and 17-beta-estradiol. Regulates the plasma metabolic clearance rate of steroid hormones by controlling their plasma concentration
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-29
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 296673 Link Image
Target 2 UniProtKB/Swiss-Prot ID P04278 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name SHBG_HUMAN Link Image
Target 2 PDB ID 1F5F Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Secreted protein. In testis, it is synthesized by the Sertoli cells, secreted into the lumen of the
Target 2 Gene Sequence >1209 bp 
ATGGAGAGCAGAGGCCCACTGGCTACCTCGCGCCTGCTGCTGTTGCTGCTGTTGCTACTA
CTGCGTCACACCCGCCAGGGATGGGCCCTGAGACCTGTTCTCCCCACCCAGAGTGCCCAC
GACCCTCCGGCTGTCCACCTCAGCAATGGCCCAGGACAAGAGCCTATCGCTGTCATGACC
TTTGACCTCACCAAGATCACAAAAACCTCCTCCTCCTTTGAGGTTCGAACCTGGGACCCA
GAGGGAGTGATTTTTTATGGGGATACCAACCCTAAGGATGACTGGTTTATGCTGGGACTT
CGAGACGGCAGGCCTGAGATCCAACTGCACAATCACTGGGCCCAGCTTACGGTGGGTGCT
GGACCACGGCTGGATGATGGGAGATGGCACCAGGTGGAAGTCAAGATGGAGGGGGACTCT
GTGCTGCTGGAGGTGGATGGGGAGGAGGTGCTGCGCCTGAGACAGGTCTCTGGGCCCCTG
ACCAGCAAACGCCATCCCATCATGAGGATTGCGCTTGGGGGGCTGCTCTTCCCCGCTTCC
AACCTTCGGTTGCCGCTGGTTCCTGCCCTGGATGGCTGCCTGCGCCGGGATTCCTGGCTG
GACAAACAGGCCGAGATCTCAGCATCTGCCCCCACTAGCCTCAGAAGCTGTGATGTAGAA
TCAAATCCCGGGATATTTCTCCCTCCAGGGACTCAGGCAGAATTCAATCTCCGAGACATT
CCCCAGCCTCATGCAGAGCCCTGGGCCTTCTCTTTGGACCTGGGACTCAAGCAGGCAGCA
GGCTCAGGCCACCTCCTTGCTCTTGGGACACCAGAGAACCCATCTTGGCTCAGTCTCCAC
CTCCAAGATCAAAAGGTGGTGTTGTCTTCTGGGTCGGGGCCAGGGCTGGATCTGCCCCTG
GTCTTGGGACTCCCTCTTCAGCTGAAGCTGAGTATGTCCAGGGTGGTCTTGAGCCAAGGG
TCGAAGATGAAGGCCCTTGCCCTGCCTCCCTTAGGCCTGGCTCCCCTCCTTAACCTCTGG
GCCAAGCCTCAAGGGCGTCTCTTCCTGGGGGCTTTACCAGGAGAAGACTCTTCCACCTCT
TTTTGCCTGAATGGCCTTTGGGCACAAGGTCAGAGGCTGGATGTGGACCAGGCCCTGAAC
AGAAGCCATGAGATCTGGACTCACAGCTGCCCCCAGAGCCCAGGCAATGGCACTGACGCT
TCCCATTAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID SHBG Link Image
Target 2 GenAtlas ID SHBG Link Image
Target 2 HGNC ID HGNC:10839 Link Image
Target 2 Chromosome Location 17
Target 2 Locus 17p13-p12
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Grishkovskaya I, Avvakumov GV, Sklenar G, Dales D, Hammond GL, Muller YA: Crystal structure of human sex hormone-binding globulin: steroid transport by a laminin G-like domain. EMBO J. 2000 Feb 15;19(4):504-12. [PubMed Link Image]
  3. Grishkovskaya I, Avvakumov GV, Hammond GL, Catalano MG, Muller YA: Steroid ligands bind human sex hormone-binding globulin in specific orientations and produce distinct changes in protein conformation. J Biol Chem. 2002 Aug 30;277(35):32086-93. Epub 2002 Jun 13. [PubMed Link Image]
  4. Power SG, Bocchinfuso WP, Pallesen M, Warmels-Rodenhiser S, Van Baelen H, Hammond GL: Molecular analyses of a human sex hormone-binding globulin variant: evidence for an additional carbohydrate chain. J Clin Endocrinol Metab. 1992 Oct;75(4):1066-70. [PubMed Link Image]
  5. Gershagen S, Lundwall A, Fernlund P: Characterization of the human sex hormone binding globulin (SHBG) gene and demonstration of two transcripts in both liver and testis. Nucleic Acids Res. 1989 Nov 25;17(22):9245-58. [PubMed Link Image]
  6. Hammond GL, Underhill DA, Rykse HM, Smith CL: The human sex hormone-binding globulin gene contains exons for androgen-binding protein and two other testicular messenger RNAs. Mol Endocrinol. 1989 Nov;3(11):1869-76. [PubMed Link Image]
  7. Que BG, Petra PH: Characterization of a cDNA coding for sex steroid-binding protein of human plasma. FEBS Lett. 1987 Jul 27;219(2):405-9. [PubMed Link Image]
  8. Gershagen S, Fernlund P, Lundwall A: A cDNA coding for human sex hormone binding globulin. Homology to vitamin K-dependent protein S. FEBS Lett. 1987 Aug 10;220(1):129-35. [PubMed Link Image]
  9. Walsh KA, Titani K, Takio K, Kumar S, Hayes R, Petra PH: Amino acid sequence of the sex steroid binding protein of human blood plasma. Biochemistry. 1986 Nov 18;25(23):7584-90. [PubMed Link Image]
  10. Hammond GL, Underhill DA, Smith CL, Goping IS, Harley MJ, Musto NA, Cheng CY, Bardin CW: The cDNA-deduced primary structure of human sex hormone-binding globulin and location of its steroid-binding domain. FEBS Lett. 1987 May 4;215(1):100-4. [PubMed Link Image]
  11. 3702459 Hammond GL, Robinson PA, Sugino H, Ward DN, Finne J: Physicochemical characteristics of human sex hormone binding globulin: evidence for two identical subunits. J Steroid Biochem. 1986 Apr;24(4):815-24.
  12. 7714097 Hardy DO, Carino C, Catterall JF, Larrea F: Molecular characterization of a genetic variant of the steroid hormone-binding globulin gene in heterozygous subjects. J Clin Endocrinol Metab. 1995 Apr;80(4):1253-6.
Target 2 Drug References
  1. Doren M, Rubig A, Coelingh Bennink HJ, Holzgreve W: Differential effects on the androgen status of postmenopausal women treated with tibolone and continuous combined estradiol and norethindrone acetate replacement therapy. Fertil Steril. 2001 Mar;75(3):554-9. [PubMed Link Image]
  2. Boyd RA, Zegarac EA, Posvar EL, Flack MR: Minimal androgenic activity of a new oral contraceptive containing norethindrone acetate and graduated doses of ethinyl estradiol. Contraception. 2001 Feb;63(2):71-6. [PubMed Link Image]
  3. Klinger G, Piater T, Jager R, Kuntzel B, Schon R, Hobe G: Non-protein bound dienogest in serum and salivary dienogest in women taking the oral contraceptives Certostat and Valette. Pharmazie. 2001 Apr;56(4):325-8. [PubMed Link Image]
  4. Nugent AG, Leung KC, Sullivan D, Reutens AT, Ho KK: Modulation by progestogens of the effects of oestrogen on hepatic endocrine function in postmenopausal women. Clin Endocrinol (Oxf). 2003 Dec;59(6):690-8. [PubMed Link Image]
  5. Saarikoski S, Yliskoski M, Penttila I: [Sequential administration of norethisterone and natural oral progesterone during premenopausal menstrual cycle disorders] Rev Fr Gynecol Obstet. 1991 Jun;86(6):475-80. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.