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Assay Detail

CHEMBL3705381

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

Binding
IMAP Assay: Cdk9/cyclinT1 is purchased from Millipore, cat #14-685. The final total protein concentration in the assay 4 nM. The 5TAMRA-cdk7tide peptide substrate, 5TAMRA-YSPTSPSYSPTSPSYSTPSPS--COOH, is purchased from Molecular Devices, cat#R7352. The final concentration of peptide substrate is 100 nM. The ATP substrate (Adenosine-5'-triphosphate) is purchased from Roche Diagnostics, cat#1140965. The final concentration of ATP substrate is 6 uM. IMAP (Immobilized Metal Assay for Phosphochemicals) Progressive Binding reagent is purchased from Molecular Devices, cat#R8139. Fluorescence polarization (FP) is used for detection. The 5TAMRA-cdk7tide peptide is phosphorylated by Cdk9/cyclinT1 kinase using the ATP substrate. The Phospho-5TAMRA-cdk7tide peptide substrate is bound to the IMAP Progressive Binding Reagent.
ChEMBL ↗
352
Total Activities
348
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-T1 (CHEMBL2108) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heteroaryl compounds and their uses
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 352 10.19 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3656855 — — 1 11.00
CHEMBL3653003 — — 1 10.98
CHEMBL3656781 — — 1 10.98
CHEMBL3652946 — — 1 10.96
CHEMBL3652958 — — 1 10.96
CHEMBL3653025 — — 1 10.96
CHEMBL3656851 — — 1 10.96
CHEMBL3652915 — — 1 10.95
CHEMBL3652923 — — 1 10.95
CHEMBL3656779 — — 1 10.94
CHEMBL3652953 — — 1 10.93
CHEMBL3653046 — — 1 10.92
CHEMBL3652896 — — 1 10.91
CHEMBL3653007 — — 1 10.90
CHEMBL3653030 — — 1 10.89
CHEMBL3653043 — — 1 10.89
CHEMBL3652912 — — 1 10.89
CHEMBL3656812 — — 1 10.88
CHEMBL3652945 — — 1 10.87
CHEMBL3656771 — — 1 10.87
CHEMBL3652954 — — 1 10.85
CHEMBL3653029 — — 1 10.85
CHEMBL3653078 — — 1 10.85
CHEMBL3652919 — — 1 10.84
CHEMBL3653001 — — 1 10.84
CHEMBL3656764 — — 1 10.83
CHEMBL3652903 — — 1 10.82
CHEMBL3653038 — — 1 10.82
CHEMBL3652976 — — 1 10.81
CHEMBL3656775 — — 1 10.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3656855 — IC50 = 0.01 nM 11.00
CHEMBL3653003 — IC50 = 0.01052 nM 10.98
CHEMBL3656781 — IC50 = 0.01058 nM 10.98
CHEMBL3652958 — IC50 = 0.011 nM 10.96
CHEMBL3656851 — IC50 = 0.011 nM 10.96
CHEMBL3652946 — IC50 = 0.01108 nM 10.96
CHEMBL3653025 — IC50 = 0.011 nM 10.96
CHEMBL3652923 — IC50 = 0.01113 nM 10.95
CHEMBL3652915 — IC50 = 0.01124 nM 10.95
CHEMBL3656779 — IC50 = 0.01154 nM 10.94
CHEMBL3652953 — IC50 = 0.01162 nM 10.93
CHEMBL3653046 — IC50 = 0.01213 nM 10.92
CHEMBL3652896 — IC50 = 0.01242 nM 10.91
CHEMBL3653007 — IC50 = 0.01255 nM 10.90
CHEMBL3653030 — IC50 = 0.013 nM 10.89
CHEMBL3652912 — IC50 = 0.01288 nM 10.89
CHEMBL3653043 — IC50 = 0.013 nM 10.89
CHEMBL3656812 — IC50 = 0.0131 nM 10.88
CHEMBL3652945 — IC50 = 0.01353 nM 10.87
CHEMBL3656771 — IC50 = 0.01363 nM 10.87
CHEMBL3653078 — IC50 = 0.0142 nM 10.85
CHEMBL3652954 — IC50 = 0.01412 nM 10.85
CHEMBL3653029 — IC50 = 0.014 nM 10.85
CHEMBL3653001 — IC50 = 0.01443 nM 10.84
CHEMBL3652919 — IC50 = 0.01443 nM 10.84
CHEMBL3656764 — IC50 = 0.01485 nM 10.83
CHEMBL3652903 — IC50 = 0.015 nM 10.82
CHEMBL3653038 — IC50 = 0.015 nM 10.82
CHEMBL3652976 — IC50 = 0.01532 nM 10.81
CHEMBL3656775 — IC50 = 0.01541 nM 10.81
CHEMBL3652978 — IC50 = 0.01582 nM 10.80
CHEMBL3653011 — IC50 = 0.01581 nM 10.80
CHEMBL3656813 — IC50 = 0.0161 nM 10.79
CHEMBL3652898 — IC50 = 0.01626 nM 10.79
CHEMBL3652936 — IC50 = 0.01713 nM 10.77
CHEMBL3653071 — IC50 = 0.01747 nM 10.76
CHEMBL3652921 — IC50 = 0.01737 nM 10.76
CHEMBL3652931 — IC50 = 0.0181 nM 10.74
CHEMBL3656846 — IC50 = 0.018 nM 10.74
CHEMBL3653033 — IC50 = 0.018 nM 10.74
CHEMBL3652975 — IC50 = 0.01809 nM 10.74
CHEMBL3656772 — IC50 = 0.01842 nM 10.73
CHEMBL3652882 — IC50 = 0.01857 nM 10.73
CHEMBL3652922 — IC50 = 0.01922 nM 10.72
CHEMBL3653068 — IC50 = 0.01884 nM 10.72
CHEMBL3653027 — IC50 = 0.019 nM 10.72
CHEMBL3653014 — IC50 = 0.01935 nM 10.71
CHEMBL3656780 — IC50 = 0.02018 nM 10.70
CHEMBL3653042 — IC50 = 0.021 nM 10.68
CHEMBL3656773 — IC50 = 0.02096 nM 10.68