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Assay Detail

CHEMBL4481538

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

Binding
Inhibition of EGFR L858R/T790M double mutant (unknown origin) by HTRF assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.
Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D.
J Med Chem (2019) 62 : 2843 -2848
PubMed 30768270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.13 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4094959 1 8.52
CHEMBL4534592 1 7.55
CHEMBL1873475 IBRUTINIB 4.0 1 7.40
CHEMBL4584630 1 6.98
CHEMBL4588202 1 6.17
CHEMBL4071151 1 6.16
CHEMBL4581088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4094959 IC50 = 3.0 nM 8.52
CHEMBL4534592 IC50 = 28.0 nM 7.55
CHEMBL1873475 IBRUTINIB IC50 = 40.0 nM 7.40
CHEMBL4584630 IC50 = 104.0 nM 6.98
CHEMBL4588202 IC50 = 677.0 nM 6.17
CHEMBL4071151 IC50 = 693.0 nM 6.16
CHEMBL4581088 IC50 > 1000.0 nM -