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Assay Detail

CHEMBL677387

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

Binding
Inhibition of phosphorylation of polyglutamic acid/tyrosine random copolymer by epidermal growth factor receptor.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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. 13. Structure-activity relationships for soluble 7-substituted 4-[(3-bromophenyl)amino]pyrido[4,3-d]pyrimidines designed as inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Thompson AM, Murray DK, Elliott WL, Fry DW, Nelson JA, Showalter HD, Roberts BJ, Vincent PW, Denny WA.
J Med Chem (1997) 40 : 3915 -3925
PubMed 9397172 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 8.55 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53428 1 10.05
CHEMBL420624 1 10.00
CHEMBL54400 1 9.89
CHEMBL127041 1 9.62
CHEMBL128468 1 9.55
CHEMBL127086 1 9.21
CHEMBL339416 1 9.13
CHEMBL126372 1 9.04
CHEMBL127058 1 8.92
CHEMBL127082 1 8.85
CHEMBL128467 1 8.85
CHEMBL338175 1 8.82
CHEMBL126623 1 8.72
CHEMBL341319 1 8.59
CHEMBL127611 1 8.49
CHEMBL128987 1 8.49
CHEMBL340700 1 8.49
CHEMBL92812 1 8.40
CHEMBL129579 1 8.32
CHEMBL340484 1 8.31
CHEMBL126384 1 8.27
CHEMBL338215 1 8.27
CHEMBL341522 1 8.25
CHEMBL340508 1 8.15
CHEMBL129825 1 8.13
CHEMBL129824 1 8.08
CHEMBL126893 1 8.06
CHEMBL435993 1 8.04
CHEMBL129509 1 8.03
CHEMBL52076 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53428 IC50 = 0.09 nM 10.05
CHEMBL420624 IC50 = 0.1 nM 10.00
CHEMBL54400 IC50 = 0.13 nM 9.89
CHEMBL127041 IC50 = 0.24 nM 9.62
CHEMBL128468 IC50 = 0.28 nM 9.55
CHEMBL127086 IC50 = 0.61 nM 9.21
CHEMBL339416 IC50 = 0.74 nM 9.13
CHEMBL126372 IC50 = 0.92 nM 9.04
CHEMBL127058 IC50 = 1.2 nM 8.92
CHEMBL127082 IC50 = 1.4 nM 8.85
CHEMBL128467 IC50 = 1.4 nM 8.85
CHEMBL338175 IC50 = 1.5 nM 8.82
CHEMBL126623 IC50 = 1.9 nM 8.72
CHEMBL341319 IC50 = 2.6 nM 8.59
CHEMBL340700 IC50 = 3.2 nM 8.49
CHEMBL127611 IC50 = 3.2 nM 8.49
CHEMBL128987 IC50 = 3.2 nM 8.49
CHEMBL92812 IC50 = 4.0 nM 8.40
CHEMBL129579 IC50 = 4.8 nM 8.32
CHEMBL340484 IC50 = 4.9 nM 8.31
CHEMBL126384 IC50 = 5.4 nM 8.27
CHEMBL338215 IC50 = 5.4 nM 8.27
CHEMBL341522 IC50 = 5.6 nM 8.25
CHEMBL340508 IC50 = 7.1 nM 8.15
CHEMBL129825 IC50 = 7.4 nM 8.13
CHEMBL129824 IC50 = 8.4 nM 8.08
CHEMBL126893 IC50 = 8.8 nM 8.06
CHEMBL435993 IC50 = 9.2 nM 8.04
CHEMBL129509 IC50 = 9.3 nM 8.03
CHEMBL52076 IC50 = 10.0 nM 8.00
CHEMBL128759 IC50 = 12.0 nM 7.92
CHEMBL125568 IC50 = 14.0 nM 7.85
CHEMBL126903 IC50 = 16.0 nM 7.80
CHEMBL126137 IC50 = 40.0 nM 7.40
CHEMBL128432 IC50 = 45.0 nM 7.35