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Assay Detail

CHEMBL3624233

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

Binding
Displacement of [3H]-DHT from androgen receptor in human MDA-MB-453 cells after 90 mins by TopCount analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Balog A, Rampulla R, Martin GS, Krystek SR, Attar R, Dell-John J, DiMarco JD, Fairfax D, Gougoutas J, Holst CL, Nation A, Rizzo C, Rossiter LM, Schweizer L, Shan W, Spergel S, Spires T, Cornelius G, Gottardis M, Trainor G, Vite GD, Salvati ME.
ACS Med Chem Lett (2015) 6 : 908 -912
PubMed 26288692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.83 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623125 1 9.00
CHEMBL3623127 1 8.77
CHEMBL3623126 1 8.70
CHEMBL3623119 1 8.52
CHEMBL3623122 1 8.15
CHEMBL3623114 1 8.10
CHEMBL3623124 1 8.00
CHEMBL3623123 1 7.92
CHEMBL3623116 1 7.64
CHEMBL3623118 1 7.51
CHEMBL3623121 1 7.51
CHEMBL3623117 1 7.30
CHEMBL3623120 1 7.30
CHEMBL409 BICALUTAMIDE 4.0 1 7.19
CHEMBL3623115 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623125 Ki = 1.0 nM 9.00
CHEMBL3623127 Ki = 1.7 nM 8.77
CHEMBL3623126 Ki = 2.0 nM 8.70
CHEMBL3623119 Ki = 3.0 nM 8.52
CHEMBL3623122 Ki = 7.0 nM 8.15
CHEMBL3623114 Ki = 8.0 nM 8.10
CHEMBL3623124 Ki = 10.0 nM 8.00
CHEMBL3623123 Ki = 12.0 nM 7.92
CHEMBL3623116 Ki = 23.0 nM 7.64
CHEMBL3623118 Ki = 31.0 nM 7.51
CHEMBL3623121 Ki = 31.0 nM 7.51
CHEMBL3623117 Ki = 50.0 nM 7.30
CHEMBL3623120 Ki = 50.0 nM 7.30
CHEMBL409 BICALUTAMIDE Ki = 64.0 nM 7.19
CHEMBL3623115 Ki = 1600.0 nM 5.80