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Assay Detail

CHEMBL687469

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Functional
Inhibition of HCT116 colon carcinoma cell proliferation
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Expert

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Yue EW, Higley CA, DiMeo SV, Carini DJ, Nugiel DA, Benware C, Benfield PA, Burton CR, Cox S, Grafstrom RH, Sharp DM, Sisk LM, Boylan JF, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Seitz SP, Trainor GL.
J Med Chem (2002) 45 : 5233 -5248
PubMed 12431051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.99 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL149096 1 7.54
CHEMBL148638 1 7.39
CHEMBL356728 1 7.19
CHEMBL148995 1 7.13
CHEMBL358525 1 6.96
CHEMBL149450 1 6.92
CHEMBL151546 1 6.89
CHEMBL148669 1 6.85
CHEMBL359200 1 6.54
CHEMBL150867 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL149096 IC50 = 29.0 nM 7.54
CHEMBL148638 IC50 = 41.0 nM 7.39
CHEMBL356728 IC50 = 64.0 nM 7.19
CHEMBL148995 IC50 = 74.0 nM 7.13
CHEMBL358525 IC50 = 110.0 nM 6.96
CHEMBL149450 IC50 = 120.0 nM 6.92
CHEMBL151546 IC50 = 130.0 nM 6.89
CHEMBL148669 IC50 = 140.0 nM 6.85
CHEMBL359200 IC50 = 290.0 nM 6.54
CHEMBL150867 IC50 = 360.0 nM 6.44