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Assay Detail

CHEMBL4388526

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

ADMET
Inhibition of probe binding to wild type EGFR (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
Mansour TS, Potluri V, Pallepati RR, Basetti V, Keesara M, Moghudula AG, Maiti P.
Bioorg Med Chem Lett (2019) 29 : 1435 -1439
PubMed 31023512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.59 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4582933 1 7.60
CHEMBL4457885 1 7.12
CHEMBL4457447 1 6.92
CHEMBL4517633 1 6.90
CHEMBL4446124 1 6.79
CHEMBL4456266 1 6.68
CHEMBL4519470 1 6.60
CHEMBL4519305 1 6.59
CHEMBL4531250 1 6.47
CHEMBL4593016 1 6.18
CHEMBL4547475 1 6.14
CHEMBL4560998 1 5.06
CHEMBL4551202 1 -
CHEMBL4463005 1 -
CHEMBL4576802 1 -
CHEMBL4546553 1 -
CHEMBL4441244 1 -
CHEMBL4451538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4582933 IC50 = 25.0 nM 7.60
CHEMBL4457885 IC50 = 76.0 nM 7.12
CHEMBL4457447 IC50 = 120.0 nM 6.92
CHEMBL4517633 IC50 = 125.0 nM 6.90
CHEMBL4446124 IC50 = 164.0 nM 6.79
CHEMBL4456266 IC50 = 210.0 nM 6.68
CHEMBL4519470 IC50 = 253.0 nM 6.60
CHEMBL4519305 IC50 = 256.0 nM 6.59
CHEMBL4531250 IC50 = 340.0 nM 6.47
CHEMBL4593016 IC50 = 658.0 nM 6.18
CHEMBL4547475 IC50 = 730.0 nM 6.14
CHEMBL4560998 IC50 = 8630.0 nM 5.06
CHEMBL4551202 IC50 > 10000.0 nM -
CHEMBL4463005 IC50 - -
CHEMBL4576802 IC50 - -
CHEMBL4546553 IC50 - -
CHEMBL4441244 IC50 - -
CHEMBL4451538 IC50 - -