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Assay Detail

CHEMBL4394427

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Functional
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Autocuration

Target

PC-3 (CHEMBL390)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Zhang Y, Wu X, Xue X, Li C, Wang J, Wang R, Zhang C, Wang C, Shi Y, Zou L, Li Q, Huang Z, Hao X, Loomes K, Wu D, Chen HW, Xu J, Xu Y.
J Med Chem (2019) 62 : 4716 -4730
PubMed 30964293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.66 4.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4537738 1 4.95
CHEMBL4465197 1 4.91
CHEMBL4439690 1 4.72
CHEMBL4558865 1 4.66
CHEMBL2137199 1 4.61
CHEMBL4455520 1 4.51
CHEMBL1082407 ENZALUTAMIDE 4.0 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4537738 IC50 = 11140.0 nM 4.95
CHEMBL4465197 IC50 = 12360.0 nM 4.91
CHEMBL4439690 IC50 = 19250.0 nM 4.72
CHEMBL4558865 IC50 = 21840.0 nM 4.66
CHEMBL2137199 IC50 = 24820.0 nM 4.61
CHEMBL4455520 IC50 = 30880.0 nM 4.51
CHEMBL1082407 ENZALUTAMIDE IC50 = 53380.0 nM 4.27