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Assay Detail

CHEMBL1768451

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

Binding
Inhibition of Src after 10 mins by radiometric phosphate incorporation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM.
J Med Chem (2011) 54 : 2341 -2350
PubMed 21391610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.36 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738829 1 7.40
CHEMBL1765781 1 6.92
CHEMBL1765774 1 6.85
CHEMBL1765776 1 6.66
CHEMBL1765782 1 6.55
CHEMBL1765783 1 6.52
CHEMBL1765777 1 6.32
CHEMBL1765784 1 6.32
CHEMBL1765779 1 6.23
CHEMBL1765780 1 6.23
CHEMBL1765775 1 5.92
CHEMBL1765770 1 5.88
CHEMBL1765097 1 5.75
CHEMBL1765772 1 5.55
CHEMBL1765778 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738829 Ki = 40.0 nM 7.40
CHEMBL1765781 Ki = 120.0 nM 6.92
CHEMBL1765774 Ki = 140.0 nM 6.85
CHEMBL1765776 Ki = 220.0 nM 6.66
CHEMBL1765782 Ki = 280.0 nM 6.55
CHEMBL1765783 Ki = 300.0 nM 6.52
CHEMBL1765777 Ki = 480.0 nM 6.32
CHEMBL1765784 Ki = 480.0 nM 6.32
CHEMBL1765779 Ki = 590.0 nM 6.23
CHEMBL1765780 Ki = 590.0 nM 6.23
CHEMBL1765775 Ki = 1200.0 nM 5.92
CHEMBL1765770 Ki = 1320.0 nM 5.88
CHEMBL1765097 Ki = 1800.0 nM 5.75
CHEMBL1765772 Ki = 2800.0 nM 5.55
CHEMBL1765778 Ki > 4000.0 nM -