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Assay Detail

CHEMBL5522786

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

Functional
Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

LNCaP (CHEMBL612518)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer.
Chen Z, Wang M, Wu D, Zhao L, Metwally H, Jiang W, Wang Y, Bai L, McEachern D, Luo J, Wang M, Li Q, Matvekas A, Wen B, Sun D, Chinnaiyan AM, Wang S.
J Med Chem (2024) 67 : 5351 -5372
PubMed 38530938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.47 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5562164 1 8.80
CHEMBL4862963 BAVDEGALUTAMIDE 1.0 1 6.91
CHEMBL4785363 INOBRODIB 1.0 1 6.38
CHEMBL4076748 1 5.16
CHEMBL1082407 ENZALUTAMIDE 4.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5562164 IC50 = 1.6 nM 8.80
CHEMBL4862963 BAVDEGALUTAMIDE IC50 = 124.0 nM 6.91
CHEMBL4785363 INOBRODIB IC50 = 412.0 nM 6.38
CHEMBL4076748 IC50 = 7000.0 nM 5.16
CHEMBL1082407 ENZALUTAMIDE IC50 = 8000.0 nM 5.10