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Assay Detail

CHEMBL648322

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

Binding
Binding affinity against Androgen receptor transfected into COS cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
Edwards JP, West SJ, Pooley CL, Marschke KB, Farmer LJ, Jones TK.
Bioorg Med Chem Lett (1998) 8 : 745 -750
PubMed 9871534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.64 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL163425 1 8.40
CHEMBL350932 1 8.30
CHEMBL162569 1 8.22
CHEMBL351519 1 8.05
CHEMBL163366 1 8.05
CHEMBL422196 1 8.05
CHEMBL161892 1 8.00
CHEMBL348918 1 8.00
CHEMBL351465 1 8.00
CHEMBL349229 1 7.77
CHEMBL165219 1 7.68
CHEMBL351447 1 7.68
CHEMBL166212 1 7.64
CHEMBL351022 1 7.55
CHEMBL349631 1 7.48
CHEMBL165912 1 7.20
CHEMBL423620 1 7.11
CHEMBL161980 1 7.11
CHEMBL409 BICALUTAMIDE 4.0 1 7.09
CHEMBL165803 1 7.03
CHEMBL163143 1 7.01
CHEMBL352456 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL163425 Ki = 4.0 nM 8.40
CHEMBL350932 Ki = 5.0 nM 8.30
CHEMBL162569 Ki = 6.0 nM 8.22
CHEMBL351519 Ki = 9.0 nM 8.05
CHEMBL163366 Ki = 9.0 nM 8.05
CHEMBL422196 Ki = 9.0 nM 8.05
CHEMBL161892 Ki = 10.0 nM 8.00
CHEMBL348918 Ki = 10.0 nM 8.00
CHEMBL351465 Ki = 10.0 nM 8.00
CHEMBL349229 Ki = 17.0 nM 7.77
CHEMBL165219 Ki = 21.0 nM 7.68
CHEMBL351447 Ki = 21.0 nM 7.68
CHEMBL166212 Ki = 23.0 nM 7.64
CHEMBL351022 Ki = 28.0 nM 7.55
CHEMBL349631 Ki = 33.0 nM 7.48
CHEMBL165912 Ki = 63.0 nM 7.20
CHEMBL423620 Ki = 77.0 nM 7.11
CHEMBL161980 Ki = 78.0 nM 7.11
CHEMBL409 BICALUTAMIDE Ki = 82.0 nM 7.09
CHEMBL165803 Ki = 94.0 nM 7.03
CHEMBL163143 Ki = 97.0 nM 7.01
CHEMBL352456 Ki = 194.0 nM 6.71