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Assay Detail

CHEMBL4180591

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Functional
Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COLO 205
Confidence 1 — Organism
Curated By Intermediate

Target

COLO 205 (CHEMBL614561)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.
Fu Y, Tang S, Su Y, Lan X, Ye Y, Zha C, Li L, Cao J, Chen Y, Jiang L, Huang Y, Ding J, Geng M, Huang M, Wan H.
Bioorg Med Chem Lett (2017) 27 : 5332 -5336
PubMed 29074254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.48 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218267 1 7.40
CHEMBL4204030 1 7.30
CHEMBL4213557 1 6.96
CHEMBL4208198 1 6.85
CHEMBL4214634 1 6.85
CHEMBL4202432 1 6.85
CHEMBL4216534 1 6.80
CHEMBL4208504 1 6.68
CHEMBL4214898 1 6.58
CHEMBL4207218 1 6.50
CHEMBL4205366 1 6.47
CHEMBL4208875 1 6.34
CHEMBL3301610 ABEMACICLIB 4.0 1 6.34
CHEMBL4214123 1 6.28
CHEMBL4218705 1 6.28
CHEMBL4211162 1 6.20
CHEMBL4203994 1 5.82
CHEMBL4213770 1 5.43
CHEMBL4206797 1 5.25
CHEMBL4206280 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218267 IC50 = 40.0 nM 7.40
CHEMBL4204030 IC50 = 50.0 nM 7.30
CHEMBL4213557 IC50 = 110.0 nM 6.96
CHEMBL4208198 IC50 = 140.0 nM 6.85
CHEMBL4214634 IC50 = 140.0 nM 6.85
CHEMBL4202432 IC50 = 140.0 nM 6.85
CHEMBL4216534 IC50 = 160.0 nM 6.80
CHEMBL4208504 IC50 = 210.0 nM 6.68
CHEMBL4214898 IC50 = 260.0 nM 6.58
CHEMBL4207218 IC50 = 320.0 nM 6.50
CHEMBL4205366 IC50 = 340.0 nM 6.47
CHEMBL4208875 IC50 = 460.0 nM 6.34
CHEMBL3301610 ABEMACICLIB IC50 = 460.0 nM 6.34
CHEMBL4214123 IC50 = 530.0 nM 6.28
CHEMBL4218705 IC50 = 520.0 nM 6.28
CHEMBL4211162 IC50 = 630.0 nM 6.20
CHEMBL4203994 IC50 = 1510.0 nM 5.82
CHEMBL4213770 IC50 = 3740.0 nM 5.43
CHEMBL4206797 IC50 = 5600.0 nM 5.25
CHEMBL4206280 IC50 - -