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Assay Detail

CHEMBL995846

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

Binding
Inhibition of EGFR kinase
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.
Hubbard RD, Dickerson SH, Emerson HK, Griffin RJ, Reno MJ, Hornberger KR, Rusnak DW, Wood ER, Uehling DE, Waterson AG.
Bioorg Med Chem Lett (2008) 18 : 5738 -5738
PubMed 18842405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.24 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496174 1 8.15
CHEMBL497804 1 7.85
CHEMBL517123 GSK-182497A 1 7.55
CHEMBL512076 GSK-192082A 1 7.50
CHEMBL501705 1 7.30
CHEMBL466586 1 7.30
CHEMBL495734 1 7.24
CHEMBL525805 1 7.22
CHEMBL500381 1 7.20
CHEMBL507329 GW869810X 1 7.19
CHEMBL500115 1 7.09
CHEMBL495979 1 6.96
CHEMBL497184 1 6.94
CHEMBL495733 1 6.92
CHEMBL523573 1 6.89
CHEMBL497803 1 6.85
CHEMBL500640 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496174 IC50 = 7.0 nM 8.15
CHEMBL497804 IC50 = 14.0 nM 7.85
CHEMBL517123 GSK-182497A IC50 = 28.0 nM 7.55
CHEMBL512076 GSK-192082A IC50 = 32.0 nM 7.50
CHEMBL501705 IC50 = 50.0 nM 7.30
CHEMBL466586 IC50 = 50.0 nM 7.30
CHEMBL495734 IC50 = 58.0 nM 7.24
CHEMBL525805 IC50 = 60.0 nM 7.22
CHEMBL500381 IC50 = 63.0 nM 7.20
CHEMBL507329 GW869810X IC50 = 65.0 nM 7.19
CHEMBL500115 IC50 = 81.0 nM 7.09
CHEMBL495979 IC50 = 109.0 nM 6.96
CHEMBL497184 IC50 = 115.0 nM 6.94
CHEMBL495733 IC50 = 120.0 nM 6.92
CHEMBL523573 IC50 = 130.0 nM 6.89
CHEMBL497803 IC50 = 140.0 nM 6.85
CHEMBL500640 IC50 = 141.0 nM 6.85