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Assay Detail

CHEMBL4684418

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

Binding
Inhibition of human full-length N-terminal GST/His6-tagged CDK9 (1 to 372 residues)/His6-tagged Cyclin-T1 (1 to 726 residues) expressed in sf9 cells using (YSPTSPS)2KK peptide as substrate in presence of [gamma33P]ATP
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK9/cyclin T1 (CHEMBL2111389)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.
Said MA,Eldehna WM,Nocentini A,Fahim SH,Bonardi A,Elgazar AA,Kryštof V,Soliman DH,Abdel-Aziz HA,Gratteri P,Abou-Seri SM,Supuran CT
Eur J Med Chem (2020) 189 : 112019 -112019
PubMed 31972394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.11 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215205 1 6.46
CHEMBL14762 SELICICLIB 2.0 1 5.75
CHEMBL4783101 1 -
CHEMBL4784840 1 -
CHEMBL4785207 1 -
CHEMBL4747175 1 -
CHEMBL4747600 1 -
CHEMBL4760748 1 -
CHEMBL4758858 1 -
CHEMBL4790806 1 -
CHEMBL4798487 1 -
CHEMBL1775075 1 -
CHEMBL4751980 1 -
CHEMBL4790351 1 -
CHEMBL4762561 1 -
CHEMBL4741899 1 -
CHEMBL4747714 1 -
CHEMBL4786073 1 -
CHEMBL4741017 1 -
CHEMBL4782119 1 -
CHEMBL4780776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215205 IC50 = 350.0 nM 6.46
CHEMBL14762 SELICICLIB IC50 = 1800.0 nM 5.75
CHEMBL4783101 IC50 > 25000.0 nM -
CHEMBL4784840 IC50 > 12500.0 nM -
CHEMBL4785207 IC50 > 12500.0 nM -
CHEMBL4747175 IC50 > 12500.0 nM -
CHEMBL4747600 IC50 > 12500.0 nM -
CHEMBL4760748 IC50 > 12500.0 nM -
CHEMBL4758858 IC50 > 12500.0 nM -
CHEMBL4790806 IC50 > 12500.0 nM -
CHEMBL4798487 IC50 > 12500.0 nM -
CHEMBL1775075 IC50 > 12500.0 nM -
CHEMBL4751980 IC50 > 12500.0 nM -
CHEMBL4790351 IC50 > 12500.0 nM -
CHEMBL4762561 IC50 > 12500.0 nM -
CHEMBL4741899 IC50 > 12500.0 nM -
CHEMBL4747714 IC50 > 12500.0 nM -
CHEMBL4786073 IC50 > 12500.0 nM -
CHEMBL4741017 IC50 > 12500.0 nM -
CHEMBL4782119 IC50 > 12500.0 nM -
CHEMBL4780776 IC50 > 12500.0 nM -