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Assay Detail

CHEMBL3736682

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

Binding
Inhibition of CDK9/Cyclin-T1 (unknown origin) using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 90 mins by autoradiography
10
Total Activities
10
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

Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.
Gao J, Fang C, Xiao Z, Huang L, Chen CH, Wang LT, Lee KH.
Medchemcomm (2015) 6 : 444 -454
PubMed 25914804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.93 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428690 ALVOCIDIB 3.0 1 8.34
CHEMBL3734879 1 6.48
CHEMBL3735502 1 6.11
CHEMBL3735818 1 5.76
CHEMBL3735561 1 5.70
CHEMBL3735231 1 5.61
CHEMBL3735656 1 5.59
CHEMBL3735432 1 4.95
CHEMBL3735063 1 4.81
CHEMBL3735072 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428690 ALVOCIDIB IC50 = 4.59 nM 8.34
CHEMBL3734879 IC50 = 330.0 nM 6.48
CHEMBL3735502 IC50 = 780.0 nM 6.11
CHEMBL3735818 IC50 = 1720.0 nM 5.76
CHEMBL3735561 IC50 = 2020.0 nM 5.70
CHEMBL3735231 IC50 = 2450.0 nM 5.61
CHEMBL3735656 IC50 = 2570.0 nM 5.59
CHEMBL3735432 IC50 = 11300.0 nM 4.95
CHEMBL3735063 IC50 = 15600.0 nM 4.81
CHEMBL3735072 IC50 > 10000.0 nM -