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Assay Detail

CHEMBL856253

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

Functional
Inhibitory concentration against Src-transformed fibroblast proliferation
22
Total Activities
22
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

4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors.
Berger DM, Dutia M, Birnberg G, Powell D, Boschelli DH, Wang YD, Ravi M, Yaczko D, Golas J, Lucas J, Boschelli F.
J Med Chem (2005) 48 : 5909 -5920
PubMed 16161995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.93 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196797 1 8.00
CHEMBL370633 1 7.72
CHEMBL198868 1 7.66
CHEMBL436486 1 7.55
CHEMBL195029 1 7.43
CHEMBL196889 1 7.38
CHEMBL427544 1 7.32
CHEMBL425389 1 7.30
CHEMBL198650 1 7.21
CHEMBL198084 1 7.15
CHEMBL288441 BOSUTINIB 4.0 1 7.00
CHEMBL372552 1 6.96
CHEMBL194352 1 6.75
CHEMBL335025 1 6.68
CHEMBL196411 1 6.66
CHEMBL198211 1 6.64
CHEMBL194969 1 6.58
CHEMBL197713 1 6.57
CHEMBL197744 1 6.46
CHEMBL196474 1 6.01
CHEMBL197930 1 5.80
CHEMBL197715 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196797 IC50 = 10.0 nM 8.00
CHEMBL370633 IC50 = 19.0 nM 7.72
CHEMBL198868 IC50 = 22.0 nM 7.66
CHEMBL436486 IC50 = 28.0 nM 7.55
CHEMBL195029 IC50 = 37.0 nM 7.43
CHEMBL196889 IC50 = 42.0 nM 7.38
CHEMBL427544 IC50 = 48.0 nM 7.32
CHEMBL425389 IC50 = 50.0 nM 7.30
CHEMBL198650 IC50 = 61.0 nM 7.21
CHEMBL198084 IC50 = 71.0 nM 7.15
CHEMBL288441 BOSUTINIB IC50 = 100.0 nM 7.00
CHEMBL372552 IC50 = 110.0 nM 6.96
CHEMBL194352 IC50 = 180.0 nM 6.75
CHEMBL335025 IC50 = 210.0 nM 6.68
CHEMBL196411 IC50 = 220.0 nM 6.66
CHEMBL198211 IC50 = 230.0 nM 6.64
CHEMBL194969 IC50 = 260.0 nM 6.58
CHEMBL197713 IC50 = 270.0 nM 6.57
CHEMBL197744 IC50 = 350.0 nM 6.46
CHEMBL196474 IC50 = 970.0 nM 6.01
CHEMBL197930 IC50 = 1600.0 nM 5.80
CHEMBL197715 IC50 = 2000.0 nM 5.70