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Assay Detail

CHEMBL4275367

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Functional
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Intermediate

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.
Zhao H, Hu X, Cao K, Zhang Y, Zhao K, Tang C, Feng B.
Eur J Med Chem (2018) 157 : 935 -945
PubMed 30165341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.80 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4286430 1 6.72
CHEMBL4289852 1 6.66
CHEMBL4278514 1 6.46
CHEMBL4290012 1 6.15
CHEMBL4288758 1 6.11
CHEMBL556881 1 6.03
CHEMBL560817 1 5.98
CHEMBL4281978 1 5.74
CHEMBL4281557 1 5.67
CHEMBL562104 1 5.51
CHEMBL4287981 1 5.43
CHEMBL4294376 1 5.37
CHEMBL4279646 1 5.32
CHEMBL559845 1 5.24
CHEMBL4283123 1 5.22
CHEMBL4293299 1 5.17
CHEMBL4277343 1 -
CHEMBL4292180 1 -
CHEMBL4287560 1 -
CHEMBL4294798 1 -
CHEMBL4293228 1 -
CHEMBL560818 1 -
CHEMBL1098059 1 -
CHEMBL4286071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4286430 IC50 = 190.0 nM 6.72
CHEMBL4289852 IC50 = 220.0 nM 6.66
CHEMBL4278514 IC50 = 350.0 nM 6.46
CHEMBL4290012 IC50 = 710.0 nM 6.15
CHEMBL4288758 IC50 = 780.0 nM 6.11
CHEMBL556881 IC50 = 940.0 nM 6.03
CHEMBL560817 IC50 = 1050.0 nM 5.98
CHEMBL4281978 IC50 = 1810.0 nM 5.74
CHEMBL4281557 IC50 = 2150.0 nM 5.67
CHEMBL562104 IC50 = 3100.0 nM 5.51
CHEMBL4287981 IC50 = 3720.0 nM 5.43
CHEMBL4294376 IC50 = 4300.0 nM 5.37
CHEMBL4279646 IC50 = 4770.0 nM 5.32
CHEMBL559845 IC50 = 5800.0 nM 5.24
CHEMBL4283123 IC50 = 6000.0 nM 5.22
CHEMBL4293299 IC50 = 6800.0 nM 5.17
CHEMBL4277343 IC50 - -
CHEMBL4292180 IC50 - -
CHEMBL4287560 IC50 - -
CHEMBL4294798 IC50 - -
CHEMBL4293228 IC50 - -
CHEMBL560818 IC50 - -
CHEMBL1098059 IC50 - -
CHEMBL4286071 IC50 - -