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Assay Detail

CHEMBL674020

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

Binding
Inhibition of phosphorylation of a polyglutamic acid/tyrosine random copolymer by EGFR enzyme prepared from human A431 carcinoma cell vesicles by immunoaffinity chromatography
24
Total Activities
24
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. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL, Denny WA.
J Med Chem (2000) 43 : 1380 -1397
PubMed 10753475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.71 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417478 1 9.80
CHEMBL31815 1 9.38
CHEMBL280757 1 9.16
CHEMBL285063 1 9.15
CHEMBL28418 1 9.12
CHEMBL31373 1 9.12
CHEMBL31326 1 9.11
CHEMBL31816 1 9.02
CHEMBL31570 1 9.01
CHEMBL31965 CANERTINIB 3.0 1 8.82
CHEMBL27688 1 8.82
CHEMBL31656 1 8.82
CHEMBL32079 1 8.77
CHEMBL32844 1 8.77
CHEMBL27685 1 8.74
CHEMBL31622 1 8.70
CHEMBL281543 1 8.57
CHEMBL286343 1 8.52
CHEMBL31419 1 8.44
CHEMBL31588 1 8.41
CHEMBL284326 1 8.18
CHEMBL31630 1 7.70
CHEMBL31369 1 7.57
CHEMBL283201 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417478 IC50 = 0.16 nM 9.80
CHEMBL31815 IC50 = 0.42 nM 9.38
CHEMBL280757 IC50 = 0.69 nM 9.16
CHEMBL285063 IC50 = 0.7 nM 9.15
CHEMBL28418 IC50 = 0.75 nM 9.12
CHEMBL31373 IC50 = 0.75 nM 9.12
CHEMBL31326 IC50 = 0.78 nM 9.11
CHEMBL31816 IC50 = 0.95 nM 9.02
CHEMBL31570 IC50 = 0.97 nM 9.01
CHEMBL31965 CANERTINIB IC50 = 1.5 nM 8.82
CHEMBL27688 IC50 = 1.5 nM 8.82
CHEMBL31656 IC50 = 1.5 nM 8.82
CHEMBL32079 IC50 = 1.7 nM 8.77
CHEMBL32844 IC50 = 1.7 nM 8.77
CHEMBL27685 IC50 = 1.8 nM 8.74
CHEMBL31622 IC50 = 2.0 nM 8.70
CHEMBL281543 IC50 = 2.7 nM 8.57
CHEMBL286343 IC50 = 3.0 nM 8.52
CHEMBL31419 IC50 = 3.6 nM 8.44
CHEMBL31588 IC50 = 3.9 nM 8.41
CHEMBL284326 IC50 = 6.6 nM 8.18
CHEMBL31630 IC50 = 20.0 nM 7.70
CHEMBL31369 IC50 = 27.0 nM 7.57
CHEMBL283201 IC50 = 45.0 nM 7.35