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Assay Detail

CHEMBL1768404

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Binding
Inhibition of c-SRC
5
Total Activities
5
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

Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.
Pevet I, Brulé C, Tizot A, Gohier A, Cruzalegui F, Boutin JA, Goldstein S.
Bioorg Med Chem (2011) 19 : 2517 -2528
PubMed 21459579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.77 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195029 1 9.34
CHEMBL5416410 DASATINIB 4.0 1 9.22
CHEMBL288441 BOSUTINIB 4.0 1 9.00
CHEMBL217092 SARACATINIB 3.0 1 8.57
CHEMBL571546 TIRBANIBULIN 4.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195029 IC50 = 0.46 nM 9.34
CHEMBL5416410 DASATINIB IC50 = 0.6 nM 9.22
CHEMBL288441 BOSUTINIB IC50 = 1.0 nM 9.00
CHEMBL217092 SARACATINIB IC50 = 2.7 nM 8.57
CHEMBL571546 TIRBANIBULIN IC50 = 20.0 nM 7.70