Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4820464

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

Binding
Binding affinity to wild-type androgen receptor in human LNCaP cells assessed as inhibition constant incubated for 24 hrs by Cheng-Prusoff equation analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Zhang Z, Connolly PJ, Lim HK, Pande V, Meerpoel L, Teleha C, Branch JR, Ondrus J, Hickson I, Bush T, Luistro L, Packman K, Bischoff JR, Ibrahim S, Parrett C, Chong Y, Gottardis MM, Bignan G.
J Med Chem (2021) 64 : 909 -924
PubMed 33470111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.93 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4865865 1 8.08
CHEMBL1082407 ENZALUTAMIDE 4.0 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4865865 Ki = 8.4 nM 8.08
CHEMBL1082407 ENZALUTAMIDE Ki = 17.0 nM 7.77