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Assay Detail

CHEMBL2446687

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

Binding
Inhibition of recombinant human FLAG-tagged ITK using biotinylated GST-SAM68 as substrate after 30 mins
21
Total Activities
21
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

Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Alder CM, Ambler M, Campbell AJ, Champigny AC, Deakin AM, Harling JD, Harris CA, Longstaff T, Lynn S, Maxwell AC, Mooney CJ, Scullion C, Singh OM, Smith IE, Somers DO, Tame CJ, Wayne G, Wilson C, Woolven JM.
ACS Med Chem Lett (2013) 4 : 948 -952
PubMed 24900590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.17 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441275 1 9.70
CHEMBL2441276 1 9.60
CHEMBL2441274 1 9.60
CHEMBL2441271 1 9.50
CHEMBL2441270 1 9.40
CHEMBL2441273 1 9.20
CHEMBL2441269 1 9.00
CHEMBL2441277 1 8.80
CHEMBL2441267 1 8.70
CHEMBL2441112 1 8.40
CHEMBL2441281 1 8.20
CHEMBL2441272 1 7.90
CHEMBL2441285 1 7.80
CHEMBL2441286 1 7.70
CHEMBL2441283 1 7.20
CHEMBL2441113 1 6.80
CHEMBL2441282 1 6.30
CHEMBL2441280 1 6.10
CHEMBL2441111 1 5.40
CHEMBL2441284 1 -
CHEMBL2441268 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441275 Ki = 0.1995 nM 9.70
CHEMBL2441276 Ki = 0.2512 nM 9.60
CHEMBL2441274 Ki = 0.2512 nM 9.60
CHEMBL2441271 Ki = 0.3162 nM 9.50
CHEMBL2441270 Ki = 0.3981 nM 9.40
CHEMBL2441273 Ki = 0.631 nM 9.20
CHEMBL2441269 Ki = 1.0 nM 9.00
CHEMBL2441277 Ki = 1.585 nM 8.80
CHEMBL2441267 Ki = 1.995 nM 8.70
CHEMBL2441112 Ki = 3.981 nM 8.40
CHEMBL2441281 Ki = 6.31 nM 8.20
CHEMBL2441272 Ki = 12.59 nM 7.90
CHEMBL2441285 Ki = 15.85 nM 7.80
CHEMBL2441286 Ki = 19.95 nM 7.70
CHEMBL2441283 Ki = 63.1 nM 7.20
CHEMBL2441113 Ki = 158.49 nM 6.80
CHEMBL2441282 Ki = 501.19 nM 6.30
CHEMBL2441280 Ki = 794.33 nM 6.10
CHEMBL2441111 Ki = 3981.07 nM 5.40
CHEMBL2441284 Ki > 10000.0 nM -
CHEMBL2441268 Ki > 10000.0 nM -