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Assay Detail

CHEMBL5037438

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Functional
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.
Lücking U, Kosemund D, Böhnke N, Lienau P, Siemeister G, Denner K, Bohlmann R, Briem H, Terebesi I, Bömer U, Schäfer M, Ince S, Mumberg D, Scholz A, Izumi R, Hwang S, von Nussbaum F.
J Med Chem (2021) 64 : 11651 -11674
PubMed 34264057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.95 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3973367 1 7.43
CHEMBL5087022 1 7.35
CHEMBL5074835 1 7.34
CHEMBL4589249 1 7.28
CHEMBL3962241 2 7.24
CHEMBL3960677 1 7.23
CHEMBL5075021 1 6.90
CHEMBL3897217 1 6.84
CHEMBL4793497 1 6.74
CHEMBL5083608 1 6.65
CHEMBL5092100 1 6.58
CHEMBL4286578 1 6.42
CHEMBL5075605 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3973367 IC50 = 37.0 nM 7.43
CHEMBL5087022 IC50 = 45.0 nM 7.35
CHEMBL5074835 IC50 = 46.0 nM 7.34
CHEMBL4589249 IC50 = 52.0 nM 7.28
CHEMBL3962241 IC50 = 57.0 nM 7.24
CHEMBL3960677 IC50 = 59.0 nM 7.23
CHEMBL3962241 IC50 = 64.0 nM 7.19
CHEMBL5075021 IC50 = 126.0 nM 6.90
CHEMBL3897217 IC50 = 144.0 nM 6.84
CHEMBL4793497 IC50 = 184.0 nM 6.74
CHEMBL5083608 IC50 = 226.0 nM 6.65
CHEMBL5092100 IC50 = 262.0 nM 6.58
CHEMBL4286578 IC50 = 380.0 nM 6.42
CHEMBL5075605 IC50 = 692.0 nM 6.16