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Assay Detail

CHEMBL677214

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Binding
Inhibition of Epidermal growth factor receptor autophosphorylation in A431 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A-431
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]ĭndoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.
Showalter HD, Bridges AJ, Zhou H, Sercel AD, McMichael A, Fry DW.
J Med Chem (1999) 42 : 5464 -5474
PubMed 10639288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.94 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153206 1 7.89
CHEMBL358934 1 7.48
CHEMBL153573 1 7.38
CHEMBL152905 1 7.07
CHEMBL357570 1 7.07
CHEMBL554983 1 7.03
CHEMBL155278 1 7.01
CHEMBL356850 1 6.77
CHEMBL345988 1 6.31
CHEMBL423224 1 6.20
CHEMBL152984 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153206 IC50 = 13.0 nM 7.89
CHEMBL358934 IC50 = 33.0 nM 7.48
CHEMBL153573 IC50 = 42.0 nM 7.38
CHEMBL152905 IC50 = 86.0 nM 7.07
CHEMBL357570 IC50 = 85.0 nM 7.07
CHEMBL554983 IC50 = 93.0 nM 7.03
CHEMBL155278 IC50 = 98.0 nM 7.01
CHEMBL356850 IC50 = 170.0 nM 6.77
CHEMBL345988 IC50 = 493.0 nM 6.31
CHEMBL423224 IC50 = 630.0 nM 6.20
CHEMBL152984 IC50 = 769.0 nM 6.11