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ChEMBL ligand: CHEMBL139835 (Androcur, Androcur 10, Ciproterona, Cyprostat, Cyproterone, Cyproterone 17.alpha.-acetate, Cyproterone acetate, Diane, NSC-81430, SH 714, SH-714, SH714) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1990) 33: 1919-1924 [PMID:2362269] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. | B | 9.12 | pKi | 0.76 | nM | Ki | J Med Chem (1992) 35: 2881-2890 [PMID:1495019] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes with GTP | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2004) 47: 2243-2255 [PMID:15084123] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor of rat cortical membranes without GTP | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2004) 47: 2243-2255 [PMID:15084123] |
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
GtoPdb | - | - | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1998) 41: 623-39 [PMID:9484511] |
ChEMBL | Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
ChEMBL | Antagonist activity at human AR AF2 assessed as inhibition of fluorescent-labelled D11-FxxLF peptide Co-activator to receptor by TR-FRET assay | B | 6.59 | pIC50 | 258.6 | nM | IC50 | J Med Chem (2022) 65: 2507-2521 [PMID:35077161] |
ChEMBL | Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. | F | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
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 | 7.51 | pKi | 31 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of [3H]-R-1881 binding to rat ventral prostate cytosolic androgen receptor | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2000) 43: 4629-4635 [PMID:11101354] |
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 6.2 | pIC50 | 630.96 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 7.33 | pIC50 | 47 | 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 | 6.99 | pKi | 102 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 6.65 | pIC50 | 225 | nM | IC50 | DrugMatrix in vitro pharmacology data |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 6.05 | pKi | 886 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.66 | pIC50 | 2183 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
ChEMBL | Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 8.31 | pKi | 4.84 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 7.43 | pIC50 | 37 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]