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Assay Detail

CHEMBL877110

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

Binding
Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate
ChEMBL ↗
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL3072) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Three-dimensional structure-activity relationships of nonsteroidal ligands in complex with androgen receptor ligand-binding domain.
Söderholm AA, Lehtovuori PT, Nyrönen TH.
J Med Chem (2005) 48 : 917 -925
PubMed 15715462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 70 7.32 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.55
CHEMBL296323 — — 1 9.52
CHEMBL419767 — — 1 9.15
CHEMBL425863 MIBOLERONE 2.0 1 9.12
CHEMBL179525 — — 1 9.07
CHEMBL386630 TESTOSTERONE 4.0 1 8.85
CHEMBL333745 — — 1 8.78
CHEMBL331820 — — 1 8.65
CHEMBL126154 — — 1 8.59
CHEMBL178354 — — 1 8.55
CHEMBL332571 — — 1 8.54
CHEMBL122495 — — 1 8.48
CHEMBL121940 ACETOTHIOLUTAMIDE — 1 8.31
CHEMBL421649 — — 1 8.21
CHEMBL124549 — — 1 8.16
CHEMBL127310 — — 1 8.10
CHEMBL339056 — — 1 8.03
CHEMBL125425 — — 1 7.97
CHEMBL63560 (R)-BICALUTAMIDE — 1 7.96
CHEMBL339333 — — 1 7.82
CHEMBL122510 — — 1 7.80
CHEMBL9337 RU-58841 — 1 7.59
CHEMBL366470 — — 1 7.57
CHEMBL340870 — — 1 7.49
CHEMBL178634 — — 1 7.48
CHEMBL428309 — — 1 7.43
CHEMBL178599 — — 1 7.39
CHEMBL125204 — — 1 7.30
CHEMBL123789 — — 1 7.24
CHEMBL266786 — — 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.2818 nM 9.55
CHEMBL296323 — Ki = 0.302 nM 9.52
CHEMBL419767 — Ki = 0.7079 nM 9.15
CHEMBL425863 MIBOLERONE Ki = 0.7586 nM 9.12
CHEMBL179525 — Ki = 0.8511 nM 9.07
CHEMBL386630 TESTOSTERONE Ki = 1.413 nM 8.85
CHEMBL333745 — Ki = 1.66 nM 8.78
CHEMBL331820 — Ki = 2.239 nM 8.65
CHEMBL126154 — Ki = 2.57 nM 8.59
CHEMBL178354 — Ki = 2.818 nM 8.55
CHEMBL332571 — Ki = 2.884 nM 8.54
CHEMBL122495 — Ki = 3.311 nM 8.48
CHEMBL121940 ACETOTHIOLUTAMIDE Ki = 4.898 nM 8.31
CHEMBL421649 — Ki = 6.166 nM 8.21
CHEMBL124549 — Ki = 6.918 nM 8.16
CHEMBL127310 — Ki = 7.943 nM 8.10
CHEMBL339056 — Ki = 9.333 nM 8.03
CHEMBL125425 — Ki = 10.72 nM 7.97
CHEMBL63560 (R)-BICALUTAMIDE Ki = 10.96 nM 7.96
CHEMBL339333 — Ki = 15.14 nM 7.82
CHEMBL122510 — Ki = 15.85 nM 7.80
CHEMBL9337 RU-58841 Ki = 25.7 nM 7.59
CHEMBL366470 — Ki = 26.92 nM 7.57
CHEMBL340870 — Ki = 32.36 nM 7.49
CHEMBL178634 — Ki = 33.11 nM 7.48
CHEMBL428309 — Ki = 37.15 nM 7.43
CHEMBL178599 — Ki = 40.74 nM 7.39
CHEMBL125204 — Ki = 50.12 nM 7.30
CHEMBL123789 — Ki = 57.54 nM 7.24
CHEMBL266786 — Ki = 64.57 nM 7.19
CHEMBL424787 — Ki = 64.57 nM 7.19
CHEMBL125809 — Ki = 81.28 nM 7.09
CHEMBL49615 — Ki = 81.28 nM 7.09
CHEMBL340668 — Ki = 89.13 nM 7.05
CHEMBL367155 — Ki = 91.2 nM 7.04
CHEMBL124737 — Ki = 97.72 nM 7.01
CHEMBL125649 — Ki = 100.0 nM 7.00
CHEMBL333731 — Ki = 104.71 nM 6.98
CHEMBL432658 — Ki = 120.23 nM 6.92
CHEMBL9146 — Ki = 123.03 nM 6.91
CHEMBL126155 — Ki = 123.03 nM 6.91
CHEMBL121992 — Ki = 128.82 nM 6.89
CHEMBL442019 — Ki = 128.82 nM 6.89
CHEMBL360708 — Ki = 131.83 nM 6.88
CHEMBL179585 — Ki = 131.83 nM 6.88
CHEMBL178635 — Ki = 134.9 nM 6.87
CHEMBL433754 — Ki = 141.25 nM 6.85
CHEMBL274667 — Ki = 141.25 nM 6.85
CHEMBL9447 — Ki = 151.36 nM 6.82
CHEMBL123673 — Ki = 199.53 nM 6.70