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Assay Detail

CHEMBL3380548

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

Binding
Inhibition of GST-tagged full length ITK (unknown origin) using BLK peptide as substrate after 35 mins
30
Total Activities
23
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

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

Publication

Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z.
J Med Chem (2014) 57 : 5714 -5727
PubMed 24918870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.88 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3263053 1 10.00
CHEMBL3298373 1 9.70
CHEMBL3298371 1 9.15
CHEMBL3298375 1 9.15
CHEMBL3298370 1 9.10
CHEMBL3263036 1 8.96
CHEMBL3298376 1 8.92
CHEMBL3298369 2 8.52
CHEMBL3298288 1 8.28
CHEMBL3298374 1 8.21
CHEMBL3298293 2 8.10
CHEMBL3298286 2 8.08
CHEMBL3298291 1 8.00
CHEMBL3298372 1 7.82
CHEMBL3298287 2 7.66
CHEMBL3298285 1 7.51
CHEMBL3298368 2 7.43
CHEMBL3298367 2 7.38
CHEMBL3262780 1 7.37
CHEMBL3298289 1 7.16
CHEMBL3298366 1 7.12
CHEMBL3298290 1 6.75
CHEMBL3298292 2 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3263053 Ki = 0.1 nM 10.00
CHEMBL3298373 Ki = 0.2 nM 9.70
CHEMBL3298371 Ki = 0.7 nM 9.15
CHEMBL3298375 Ki = 0.7 nM 9.15
CHEMBL3298370 Ki = 0.8 nM 9.10
CHEMBL3263036 Ki = 1.1 nM 8.96
CHEMBL3298376 Ki = 1.2 nM 8.92
CHEMBL3298369 Ki = 3.0 nM 8.52
CHEMBL3298288 Ki = 5.3 nM 8.28
CHEMBL3298374 Ki = 6.2 nM 8.21
CHEMBL3298293 Ki = 8.0 nM 8.10
CHEMBL3298286 Ki = 8.3 nM 8.08
CHEMBL3298286 Ki = 9.4 nM 8.03
CHEMBL3298291 Ki = 10.0 nM 8.00
CHEMBL3298372 Ki = 15.0 nM 7.82
CHEMBL3298287 Ki = 22.0 nM 7.66
CHEMBL3298285 Ki = 31.0 nM 7.51
CHEMBL3298368 Ki = 37.0 nM 7.43
CHEMBL3298367 Ki = 42.0 nM 7.38
CHEMBL3262780 Ki = 43.0 nM 7.37
CHEMBL3298367 Ki = 55.0 nM 7.26
CHEMBL3298289 Ki = 69.0 nM 7.16
CHEMBL3298366 Ki = 75.0 nM 7.12
CHEMBL3298287 Ki = 83.0 nM 7.08
CHEMBL3298293 Ki = 130.0 nM 6.89
CHEMBL3298290 Ki = 180.0 nM 6.75
CHEMBL3298292 Ki = 180.0 nM 6.75
CHEMBL3298368 Ki = 190.0 nM 6.72
CHEMBL3298369 Ki = 200.0 nM 6.70
CHEMBL3298292 Ki = 280.0 nM 6.55