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Assay Detail

CHEMBL871057

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Functional
Antiproliferative activity against PC3 cells
18
Total Activities
18
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 Expert

Target

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

Publication

CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation.
Mahale S, Aubry C, James Wilson A, Jenkins PR, Maréchal JD, Sutcliffe MJ, Chaudhuri B.
Bioorg Med Chem Lett (2006) 16 : 4272 -4278
PubMed 16750360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.35 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL211632 1 6.04
CHEMBL213805 1 5.21
CHEMBL209467 1 4.82
CHEMBL378617 1 4.44
CHEMBL213302 1 4.33
CHEMBL377131 1 4.26
CHEMBL211636 1 4.23
CHEMBL209972 1 4.18
CHEMBL376003 1 4.09
CHEMBL213032 1 4.07
CHEMBL212768 1 4.07
CHEMBL213036 1 4.05
CHEMBL209433 1 4.04
CHEMBL214008 1 4.04
CHEMBL213449 1 4.03
CHEMBL214188 1 4.03
CHEMBL211622 1 4.01
CHEMBL374207 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL211632 IC50 = 920.0 nM 6.04
CHEMBL213805 IC50 = 6200.0 nM 5.21
CHEMBL209467 IC50 = 15000.0 nM 4.82
CHEMBL378617 IC50 = 36000.0 nM 4.44
CHEMBL213302 IC50 = 47000.0 nM 4.33
CHEMBL377131 IC50 = 55000.0 nM 4.26
CHEMBL211636 IC50 = 59000.0 nM 4.23
CHEMBL209972 IC50 = 66000.0 nM 4.18
CHEMBL376003 IC50 = 81000.0 nM 4.09
CHEMBL213032 IC50 = 85000.0 nM 4.07
CHEMBL212768 IC50 = 86000.0 nM 4.07
CHEMBL213036 IC50 = 89000.0 nM 4.05
CHEMBL209433 IC50 = 92000.0 nM 4.04
CHEMBL214008 IC50 = 92000.0 nM 4.04
CHEMBL213449 IC50 = 94000.0 nM 4.03
CHEMBL214188 IC50 = 94000.0 nM 4.03
CHEMBL211622 IC50 = 98000.0 nM 4.01
CHEMBL374207 IC50 = 108000.0 nM -