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Assay Detail

CHEMBL5545632

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Functional
Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type VCaP
Confidence 1 — Organism
Curated By Autocuration

Target

VCaP (CHEMBL4296508)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.
Chen Z, Wang M, Wu D, Bai L, Xu T, Metwally H, Wang Y, McEachern D, Zhao L, Li R, Takyi-Williams J, Wang M, Wang L, Li Q, Wen B, Sun D, Wang S.
J Med Chem (2024) 67 : 5275 -5304
PubMed 38477974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.32 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5564627 1 8.34
CHEMBL4862963 BAVDEGALUTAMIDE 1.0 1 6.90
CHEMBL4785363 INOBRODIB 1.0 1 6.71
CHEMBL4076748 1 -
CHEMBL1082407 ENZALUTAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5564627 IC50 = 4.6 nM 8.34
CHEMBL4862963 BAVDEGALUTAMIDE IC50 = 125.0 nM 6.90
CHEMBL4785363 INOBRODIB IC50 = 195.0 nM 6.71
CHEMBL4076748 IC50 > 1000.0 nM -
CHEMBL1082407 ENZALUTAMIDE IC50 > 1000.0 nM -