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Assay Detail

CHEMBL679947

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Functional
Inhibition of phosphorylation of phospholipase C gamma1 by Epidermal growth factor receptor, from human A431 carcinoma cell vesicles
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.
Rewcastle GW, Bridges AJ, Fry DW, Rubin JR, Denny WA.
J Med Chem (1997) 40 : 1820 -1826
PubMed 9191958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.19 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53426 1 9.60
CHEMBL299622 1 9.12
CHEMBL294475 1 9.09
CHEMBL53777 1 9.02
CHEMBL53831 1 8.82
CHEMBL299881 1 8.64
CHEMBL51228 1 8.64
CHEMBL417420 1 8.54
CHEMBL416307 1 8.52
CHEMBL51854 1 8.42
CHEMBL52829 1 8.40
CHEMBL52591 1 8.37
CHEMBL53310 1 7.89
CHEMBL298931 1 7.77
CHEMBL54067 1 7.46
CHEMBL53311 1 7.09
CHEMBL52823 1 6.42
CHEMBL50027 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53426 IC50 = 0.25 nM 9.60
CHEMBL299622 IC50 = 0.76 nM 9.12
CHEMBL294475 IC50 = 0.81 nM 9.09
CHEMBL53777 IC50 = 0.95 nM 9.02
CHEMBL53831 IC50 = 1.5 nM 8.82
CHEMBL299881 IC50 = 2.3 nM 8.64
CHEMBL51228 IC50 = 2.3 nM 8.64
CHEMBL417420 IC50 = 2.9 nM 8.54
CHEMBL416307 IC50 = 3.0 nM 8.52
CHEMBL51854 IC50 = 3.8 nM 8.42
CHEMBL52829 IC50 = 4.0 nM 8.40
CHEMBL52591 IC50 = 4.3 nM 8.37
CHEMBL53310 IC50 = 13.0 nM 7.89
CHEMBL298931 IC50 = 17.0 nM 7.77
CHEMBL54067 IC50 = 35.0 nM 7.46
CHEMBL53311 IC50 = 82.0 nM 7.09
CHEMBL52823 IC50 = 380.0 nM 6.42
CHEMBL50027 IC50 = 2550.0 nM 5.59