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Assay Detail

CHEMBL3777656

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

Functional
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay
27
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.
Vymětalová L, Havlíček L, Šturc A, Skrášková Z, Jorda R, Pospíšil T, Strnad M, Kryštof V.
Eur J Med Chem (2016) 110 : 291 -301
PubMed 26851505 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.61 7.68
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3774949 1 7.68
CHEMBL3775792 1 7.62
CHEMBL3774632 2 7.57
CHEMBL3775502 1 7.29
CHEMBL3774932 2 7.28
CHEMBL3775677 1 7.23
CHEMBL3775470 1 7.21
CHEMBL3774979 1 6.88
CHEMBL518800 1 6.80
CHEMBL3775509 1 6.79
CHEMBL3775467 1 6.71
CHEMBL3775657 1 6.65
CHEMBL3775223 1 6.53
CHEMBL3775608 2 6.51
CHEMBL3775606 1 6.34
CHEMBL3774503 1 6.32
CHEMBL3775681 1 6.28
CHEMBL3775479 1 6.09
CHEMBL3774434 2 5.92
CHEMBL3775861 1 5.62
CHEMBL3774636 2 5.28
CHEMBL14762 SELICICLIB 2.0 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3774949 IC50 = 21.0 nM 7.68
CHEMBL3775792 IC50 = 24.0 nM 7.62
CHEMBL3774632 IC50 = 27.0 nM 7.57
CHEMBL3775502 IC50 = 51.0 nM 7.29
CHEMBL3774932 IC50 = 53.0 nM 7.28
CHEMBL3775677 IC50 = 59.0 nM 7.23
CHEMBL3775470 IC50 = 62.0 nM 7.21
CHEMBL3774979 IC50 = 133.0 nM 6.88
CHEMBL518800 IC50 = 160.0 nM 6.80
CHEMBL3775509 IC50 = 163.0 nM 6.79
CHEMBL3775467 IC50 = 195.0 nM 6.71
CHEMBL3775657 IC50 = 225.0 nM 6.65
CHEMBL3775223 IC50 = 295.0 nM 6.53
CHEMBL3775608 IC50 = 310.0 nM 6.51
CHEMBL3775606 IC50 = 460.0 nM 6.34
CHEMBL3774503 IC50 = 474.0 nM 6.32
CHEMBL3775681 IC50 = 530.0 nM 6.28
CHEMBL3775479 IC50 = 819.0 nM 6.09
CHEMBL3774434 IC50 = 1190.0 nM 5.92
CHEMBL3775861 IC50 = 2385.0 nM 5.62
CHEMBL3774636 IC50 = 5300.0 nM 5.28
CHEMBL14762 SELICICLIB IC50 = 12250.0 nM 4.91
CHEMBL3774434 Activity - -
CHEMBL3774632 Activity - -
CHEMBL3774932 Activity - -
CHEMBL3775608 Activity - -
CHEMBL3774636 Activity - -