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Assay Detail

CHEMBL834682

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Functional
Inhibition of c-Src transformed rat fibroblast proliferation
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.
Boschelli DH, Wu B, Barrios Sosa AC, Durutlic H, Chen JJ, Wang Y, Golas JM, Lucas J, Boschelli F.
J Med Chem (2005) 48 : 3891 -3902
PubMed 15916442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.03 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288441 BOSUTINIB 4.0 1 7.00
CHEMBL363575 1 6.70
CHEMBL195382 1 6.48
CHEMBL370473 1 6.46
CHEMBL194503 1 6.41
CHEMBL410251 1 6.38
CHEMBL194664 1 6.37
CHEMBL195419 1 6.20
CHEMBL372219 1 6.20
CHEMBL192052 1 6.16
CHEMBL364955 1 6.14
CHEMBL425382 1 6.07
CHEMBL190981 1 6.05
CHEMBL426990 1 5.92
CHEMBL194815 1 5.89
CHEMBL194992 1 5.85
CHEMBL366029 1 5.72
CHEMBL192652 1 5.62
CHEMBL373132 1 5.52
CHEMBL195523 1 5.51
CHEMBL195157 1 5.48
CHEMBL425371 1 5.40
CHEMBL365398 1 5.21
CHEMBL195046 1 -
CHEMBL192679 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288441 BOSUTINIB IC50 = 100.0 nM 7.00
CHEMBL363575 IC50 = 200.0 nM 6.70
CHEMBL195382 IC50 = 330.0 nM 6.48
CHEMBL370473 IC50 = 350.0 nM 6.46
CHEMBL194503 IC50 = 390.0 nM 6.41
CHEMBL410251 IC50 = 420.0 nM 6.38
CHEMBL194664 IC50 = 430.0 nM 6.37
CHEMBL195419 IC50 = 630.0 nM 6.20
CHEMBL372219 IC50 = 630.0 nM 6.20
CHEMBL192052 IC50 = 690.0 nM 6.16
CHEMBL364955 IC50 = 720.0 nM 6.14
CHEMBL425382 IC50 = 850.0 nM 6.07
CHEMBL190981 IC50 = 890.0 nM 6.05
CHEMBL426990 IC50 = 1200.0 nM 5.92
CHEMBL194815 IC50 = 1300.0 nM 5.89
CHEMBL194992 IC50 = 1400.0 nM 5.85
CHEMBL366029 IC50 = 1900.0 nM 5.72
CHEMBL192652 IC50 = 2400.0 nM 5.62
CHEMBL373132 IC50 = 3000.0 nM 5.52
CHEMBL195523 IC50 = 3100.0 nM 5.51
CHEMBL195157 IC50 = 3300.0 nM 5.48
CHEMBL425371 IC50 = 4000.0 nM 5.40
CHEMBL365398 IC50 = 6200.0 nM 5.21
CHEMBL195046 IC50 > 10000.0 nM -
CHEMBL192679 IC50 > 10000.0 nM -