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Assay Detail

CHEMBL1909115

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 6.20 8.64
Ki 871 6.37 8.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 2 8.81
CHEMBL757 NANDROLONE 3.0 2 8.68
CHEMBL386630 TESTOSTERONE 4.0 2 8.39
CHEMBL1395 METHYLTESTOSTERONE 4.0 2 8.37
CHEMBL2107797 NORGESTREL 4.0 2 8.37
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 2 8.31
CHEMBL1276308 MIFEPRISTONE 4.0 2 8.26
CHEMBL282575 ESTRADIOL BENZOATE 2.0 2 8.16
CHEMBL1479 DANAZOL 4.0 2 8.10
CHEMBL1162 NORETHINDRONE 4.0 2 7.82
CHEMBL2079587 STANOZOLOL 4.0 2 7.82
CHEMBL1200623 ETHYLESTRENOL 4.0 2 7.75
CHEMBL1201139 MEGESTROL ACETATE 4.0 2 7.70
CHEMBL110691 CHLORMADINONE ACETATE 4.0 2 7.68
CHEMBL139835 CYPROTERONE ACETATE 3.0 2 7.51
CHEMBL241694 ETHISTERONE 3.0 2 7.36
CHEMBL1201146 NORETHINDRONE ACETATE 4.0 2 7.15
CHEMBL2103774 TIBOLONE 3.0 2 7.12
CHEMBL1390 2 7.04
CHEMBL1393 SPIRONOLACTONE 4.0 2 7.04
CHEMBL1200585 OXYMETHOLONE 4.0 2 6.86
CHEMBL103 PROGESTERONE 4.0 2 6.84
CHEMBL135 ESTRADIOL 4.0 2 6.63
CHEMBL1062 HYDROXYPROGESTERONE 2 6.31
CHEMBL63560 (R)-BICALUTAMIDE 2 6.27
CHEMBL1200845 HALCINONIDE 4.0 2 6.23
CHEMBL1200600 FLUOROMETHOLONE 4.0 2 6.07
CHEMBL1370 BUDESONIDE 4.0 2 5.96
CHEMBL691 ETHINYL ESTRADIOL 4.0 2 5.96
CHEMBL577294 2-HYDROXYPROPYL-BETA-CYCLODEXTRIN 3.0 2 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 1.537 nM 8.81
CHEMBL757 NANDROLONE Ki = 2.099 nM 8.68
CHEMBL27769 STANOLONE IC50 = 2.305 nM 8.64
CHEMBL757 NANDROLONE IC50 = 3.149 nM 8.50
CHEMBL386630 TESTOSTERONE Ki = 4.112 nM 8.39
CHEMBL2107797 NORGESTREL Ki = 4.266 nM 8.37
CHEMBL1395 METHYLTESTOSTERONE Ki = 4.266 nM 8.37
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 4.839 nM 8.31
CHEMBL1276308 MIFEPRISTONE Ki = 5.563 nM 8.26
CHEMBL386630 TESTOSTERONE IC50 = 6.169 nM 8.21
CHEMBL2107797 NORGESTREL IC50 = 6.399 nM 8.19
CHEMBL1395 METHYLTESTOSTERONE IC50 = 6.399 nM 8.19
CHEMBL282575 ESTRADIOL BENZOATE Ki = 6.981 nM 8.16
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 7.259 nM 8.14
CHEMBL1479 DANAZOL Ki = 7.99 nM 8.10
CHEMBL1276308 MIFEPRISTONE IC50 = 8.345 nM 8.08
CHEMBL282575 ESTRADIOL BENZOATE IC50 = 10.0 nM 8.00
CHEMBL1479 DANAZOL IC50 = 12.0 nM 7.92
CHEMBL2079587 STANOZOLOL Ki = 15.0 nM 7.82
CHEMBL1162 NORETHINDRONE Ki = 15.0 nM 7.82
CHEMBL1200623 ETHYLESTRENOL Ki = 18.0 nM 7.75
CHEMBL1201139 MEGESTROL ACETATE Ki = 20.0 nM 7.70
CHEMBL110691 CHLORMADINONE ACETATE Ki = 20.9 nM 7.68
CHEMBL2079587 STANOZOLOL IC50 = 22.0 nM 7.66
CHEMBL1162 NORETHINDRONE IC50 = 22.0 nM 7.66
CHEMBL1200623 ETHYLESTRENOL IC50 = 27.0 nM 7.57
CHEMBL1201139 MEGESTROL ACETATE IC50 = 30.0 nM 7.52
CHEMBL139835 CYPROTERONE ACETATE Ki = 31.0 nM 7.51
CHEMBL110691 CHLORMADINONE ACETATE IC50 = 31.3 nM 7.50
CHEMBL241694 ETHISTERONE Ki = 44.0 nM 7.36
CHEMBL139835 CYPROTERONE ACETATE IC50 = 47.0 nM 7.33
CHEMBL241694 ETHISTERONE IC50 = 67.0 nM 7.17
CHEMBL1201146 NORETHINDRONE ACETATE Ki = 71.0 nM 7.15
CHEMBL2103774 TIBOLONE Ki = 75.4 nM 7.12
CHEMBL1393 SPIRONOLACTONE Ki = 90.6 nM 7.04
CHEMBL1390 Ki = 91.0 nM 7.04
CHEMBL1201146 NORETHINDRONE ACETATE IC50 = 106.0 nM 6.97
CHEMBL2103774 TIBOLONE IC50 = 113.0 nM 6.95
CHEMBL1393 SPIRONOLACTONE IC50 = 135.9 nM 6.87
CHEMBL1390 IC50 = 137.0 nM 6.86
CHEMBL1200585 OXYMETHOLONE Ki = 137.0 nM 6.86
CHEMBL103 PROGESTERONE Ki = 143.0 nM 6.84
CHEMBL1200585 OXYMETHOLONE IC50 = 206.0 nM 6.69
CHEMBL103 PROGESTERONE IC50 = 214.0 nM 6.67
CHEMBL135 ESTRADIOL Ki = 235.0 nM 6.63
CHEMBL135 ESTRADIOL IC50 = 353.0 nM 6.45
CHEMBL1062 HYDROXYPROGESTERONE Ki = 493.0 nM 6.31
CHEMBL63560 (R)-BICALUTAMIDE Ki = 534.0 nM 6.27
CHEMBL1200845 HALCINONIDE Ki = 590.0 nM 6.23
CHEMBL1062 HYDROXYPROGESTERONE IC50 = 739.0 nM 6.13