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Assay Detail

CHEMBL947134

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

Binding
Inhibition of human recombinant CDK9/cyclin T expressed in insect cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
Echalier A, Bettayeb K, Ferandin Y, Lozach O, Clément M, Valette A, Liger F, Marquet B, Morris JC, Endicott JA, Joseph B, Meijer L.
J Med Chem (2008) 51 : 737 -751
PubMed 18232649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.11 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406463 MERIOLIN 6 1 8.25
CHEMBL270687 MERIOLIN 5 1 8.25
CHEMBL270686 MERIOLIN 3 1 8.22
CHEMBL406464 MERIOLIN 4 1 8.15
CHEMBL270897 MERIOLIN 2 1 7.75
CHEMBL411704 1 7.58
CHEMBL405665 MERIOLIN 1 1 7.58
CHEMBL271597 1 7.30
CHEMBL402443 1 6.66
CHEMBL405200 1 6.60
CHEMBL271195 1 6.00
CHEMBL270926 1 5.96
CHEMBL406102 MERIOLIN 8 1 5.92
CHEMBL405074 MERIOLIN 7 1 5.28
CHEMBL270346 MERIOLIN 9 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406463 MERIOLIN 6 IC50 = 5.6 nM 8.25
CHEMBL270687 MERIOLIN 5 IC50 = 5.6 nM 8.25
CHEMBL270686 MERIOLIN 3 IC50 = 6.0 nM 8.22
CHEMBL406464 MERIOLIN 4 IC50 = 7.0 nM 8.15
CHEMBL270897 MERIOLIN 2 IC50 = 18.0 nM 7.75
CHEMBL411704 IC50 = 26.0 nM 7.58
CHEMBL405665 MERIOLIN 1 IC50 = 26.0 nM 7.58
CHEMBL271597 IC50 = 50.0 nM 7.30
CHEMBL402443 IC50 = 220.0 nM 6.66
CHEMBL405200 IC50 = 250.0 nM 6.60
CHEMBL271195 IC50 = 1000.0 nM 6.00
CHEMBL270926 IC50 = 1100.0 nM 5.96
CHEMBL406102 MERIOLIN 8 IC50 = 1200.0 nM 5.92
CHEMBL405074 MERIOLIN 7 IC50 = 5300.0 nM 5.28
CHEMBL270346 MERIOLIN 9 IC50 > 10000.0 nM -