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Assay Detail

CHEMBL5733989

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Binding
Omnia Assay: ITK: This example describes continuous-read kinase assays to measure inherent potency of compound against active forms of ITK enzymes as described in Example 251 above except that the modified ITK-optimized reagent conditions are:[ITK]=10 nM, [ATP]=25 [Y6-Sox]=10 μM (ATP KMapp=33 μM).
429
Total Activities
140
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ITK/TSK (CHEMBL2959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 2,4-diaminopyrimidines as kinase inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 143 6.99 7.26
kon 143 - -
k_off 143 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6033285 3 7.26
CHEMBL5942546 3 7.26
CHEMBL5759845 3 7.26
CHEMBL6052028 3 7.26
CHEMBL5741005 3 7.26
CHEMBL6039812 3 7.26
CHEMBL6025850 3 7.26
CHEMBL5954027 3 7.26
CHEMBL6014788 3 7.26
CHEMBL5833997 3 7.26
CHEMBL6056251 3 7.26
CHEMBL5763010 3 7.26
CHEMBL5773640 3 7.26
CHEMBL6044013 3 7.26
CHEMBL6022830 6 7.26
CHEMBL6013487 3 7.26
CHEMBL5746419 3 7.26
CHEMBL5939316 3 7.26
CHEMBL5995813 3 7.26
CHEMBL6025324 3 7.26
CHEMBL5950512 3 7.26
CHEMBL5948101 3 7.26
CHEMBL5900800 3 7.26
CHEMBL5747706 3 7.26
CHEMBL5756489 3 7.26
CHEMBL5795317 3 7.26
CHEMBL5798780 3 7.26
CHEMBL5791105 3 7.26
CHEMBL5780712 3 7.26
CHEMBL5764023 3 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5773640 IC50 = 55.0 nM 7.26
CHEMBL5821130 IC50 = 55.0 nM 7.26
CHEMBL5892354 IC50 = 55.0 nM 7.26
CHEMBL6022830 IC50 = 55.0 nM 7.26
CHEMBL5900800 IC50 = 55.0 nM 7.26
CHEMBL5891594 IC50 = 55.0 nM 7.26
CHEMBL5747706 IC50 = 55.0 nM 7.26
CHEMBL5808700 IC50 = 55.0 nM 7.26
CHEMBL5891594 IC50 = 55.0 nM 7.26
CHEMBL5756489 IC50 = 55.0 nM 7.26
CHEMBL5780633 IC50 = 55.0 nM 7.26
CHEMBL5791105 IC50 = 55.0 nM 7.26
CHEMBL5985220 IC50 = 55.0 nM 7.26
CHEMBL6033285 IC50 = 55.0 nM 7.26
CHEMBL5780712 IC50 = 55.0 nM 7.26
CHEMBL5916856 IC50 = 55.0 nM 7.26
CHEMBL6040634 IC50 = 55.0 nM 7.26
CHEMBL5763010 IC50 = 55.0 nM 7.26
CHEMBL6056251 IC50 = 55.0 nM 7.26
CHEMBL5752981 IC50 = 55.0 nM 7.26
CHEMBL6013487 IC50 = 55.0 nM 7.26
CHEMBL5797771 IC50 = 55.0 nM 7.26
CHEMBL5940517 IC50 = 55.0 nM 7.26
CHEMBL5741005 IC50 = 55.0 nM 7.26
CHEMBL6052028 IC50 = 55.0 nM 7.26
CHEMBL5970361 IC50 = 55.0 nM 7.26
CHEMBL5822224 IC50 = 55.0 nM 7.26
CHEMBL5918405 IC50 = 55.0 nM 7.26
CHEMBL6025324 IC50 = 55.0 nM 7.26
CHEMBL5858035 IC50 = 55.0 nM 7.26
CHEMBL5950214 IC50 = 55.0 nM 7.26
CHEMBL5950512 IC50 = 55.0 nM 7.26
CHEMBL5954027 IC50 = 55.0 nM 7.26
CHEMBL5740925 IC50 = 55.0 nM 7.26
CHEMBL6003257 IC50 = 55.0 nM 7.26
CHEMBL5942546 IC50 = 55.0 nM 7.26
CHEMBL5995813 IC50 = 55.0 nM 7.26
CHEMBL5939316 IC50 = 55.0 nM 7.26
CHEMBL5759845 IC50 = 55.0 nM 7.26
CHEMBL6014788 IC50 = 55.0 nM 7.26
CHEMBL5922445 IC50 = 55.0 nM 7.26
CHEMBL5933081 IC50 = 55.0 nM 7.26
CHEMBL5825514 IC50 = 55.0 nM 7.26
CHEMBL3301625 SPEBRUTINIB IC50 = 55.0 nM 7.26
CHEMBL5836521 IC50 = 55.0 nM 7.26
CHEMBL6041177 IC50 = 55.0 nM 7.26
CHEMBL5746419 IC50 = 55.0 nM 7.26
CHEMBL5833997 IC50 = 55.0 nM 7.26
CHEMBL5948101 IC50 = 55.0 nM 7.26
CHEMBL5932966 IC50 = 55.0 nM 7.26