norethisterone [Ligand Id: 2880] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1162 (Heather, Primolut N, Norlutate, Aygestin, SC-4640, Combipatch, Micronor HRT, Utovlan, NSC-9564, Noriday, Camila, Nor-Qd, Activella, Femhrt, Norlutin, Errin, Menzol, Norethisterone, Incassia, Jencycla, Norethindrone, Norethidrone, Micronor)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
  • This target only has 1 pki data point
1 CHEMBL1162_lig_chart_1 Androgen Receptor Rat
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
  • This target only has 1 pki data point
2 CHEMBL1162_lig_chart_2 Estrogen receptor alpha Human
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  • Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
  • This target only has 1 pki data point
3 CHEMBL1162_lig_chart_3 Glucocorticoid receptor Human
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4 CHEMBL1162_lig_chart_4 Progesterone receptor HumanBovine
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
  • This target only has 1 pki data point
5 CHEMBL1162_lig_chart_5 Serotonin transporter Human
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
  • This target only has 0 pki data point
6 CHEMBL1162_lig_chart_6 Testis-specific androgen-binding protein Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 7.82 pKi 15 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 6.92 pIC50 120.23 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 7.66 pIC50 22 nM IC50 DrugMatrix in vitro pharmacology data
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 6.64 pKi 231 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 6.09 pIC50 808 nM IC50 DrugMatrix in vitro pharmacology data
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 6.71 pKi 197 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 6.36 pIC50 433 nM IC50 DrugMatrix in vitro pharmacology data
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Dissociation constant for progesterone receptor B 9.4 pKd 0.4 nM Kd J. Med. Chem. (2004) 47: 3381-3387 [PMID:15189034]
ChEMBL The binding affinity measured using baculovirus-expressed hPR-A in sf21 cells. B 8.73 pKi 1.87 nM Ki J. Med. Chem. (1998) 41: 303-310 [PMID:9464361]
ChEMBL Binding affinity against Progesterone receptor in human TE85 osteosarcoma cells was determined using (Z)-[125I]-17-alpha-(2-iodovinyl)-19-nor-testosterone as radioligand B 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (1995) 38: 4880-4884 [PMID:8523400]
ChEMBL Agonistic activity was measured for modulation of hPR-B (human progesterone receptor) in co-transfected CV-1 cells. F 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (1998) 41: 303-310 [PMID:9464361]
GtoPdb - - 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (1998) 41: 303-10 [PMID:9464361]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 8.91 pKi 1.22 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 8.03 pIC50 9.34 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.62 pKi 2411 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.34 pIC50 4537 nM IC50 DrugMatrix in vitro pharmacology data
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
ChEMBL Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin B 7.97 pKd 10.72 nM Kd J. Med. Chem. (2008) 51: 2047-2056 [PMID:18330978]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]