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Assay Detail

CHEMBL5238847

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

Binding
Inhibition of mouse EGFR D770_N771insNPG mutant stably expressed in mouse BaF3 cells assessed as cell viability incubated for 3 days by Cell Titer-Glo assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BaF3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Huang WS, Li F, Gong Y, Zhang Y, Youngsaye W, Xu Y, Zhu X, Greenfield MT, Kohlmann A, Taslimi PM, Toms A, Zech SG, Zhou T, Das B, Jang HG, Tugnait M, Ye YE, Gonzalvez F, Baker TE, Nadworny S, Ning Y, Wardwell SD, Zhang S, Gould AE, Hu Y, Lane W, Skene RJ, Zou H, Clackson T, Narasimhan NI, Rivera VM, Dalgarno DC, Shakespeare WC.
Bioorg Med Chem Lett (2023) 80 : 129084 -129084
PubMed 36423823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.83 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5266100 1 8.52
CHEMBL4650319 MOBOCERTINIB 4.0 1 8.40
CHEMBL5283216 1 8.40
CHEMBL5266798 1 8.30
CHEMBL5281266 1 8.30
CHEMBL5290929 1 8.22
CHEMBL5268143 1 8.22
CHEMBL5270000 1 8.21
CHEMBL5275712 1 8.19
CHEMBL5279794 1 8.18
CHEMBL5286091 1 8.18
CHEMBL5270335 1 8.10
CHEMBL5284486 1 8.10
CHEMBL5271640 1 8.05
CHEMBL5273438 1 8.05
CHEMBL5279491 1 8.01
CHEMBL5271718 1 7.96
CHEMBL5266834 1 7.96
CHEMBL5284387 1 7.89
CHEMBL5272345 1 7.85
CHEMBL5284255 1 7.82
CHEMBL5266482 1 7.66
CHEMBL5281203 1 7.64
CHEMBL3353404 1 7.50
CHEMBL1173655 AFATINIB 4.0 1 7.44
CHEMBL5276760 1 7.42
CHEMBL5291010 1 7.28
CHEMBL5266896 1 7.28
CHEMBL3353410 OSIMERTINIB 4.0 1 7.28
CHEMBL4104658 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5266100 IC50 = 3.0 nM 8.52
CHEMBL4650319 MOBOCERTINIB IC50 = 4.0 nM 8.40
CHEMBL5283216 IC50 = 3.99 nM 8.40
CHEMBL5266798 IC50 = 5.0 nM 8.30
CHEMBL5281266 IC50 = 4.95 nM 8.30
CHEMBL5290929 IC50 = 6.0 nM 8.22
CHEMBL5268143 IC50 = 6.0 nM 8.22
CHEMBL5270000 IC50 = 6.2 nM 8.21
CHEMBL5275712 IC50 = 6.43 nM 8.19
CHEMBL5279794 IC50 = 6.57 nM 8.18
CHEMBL5286091 IC50 = 6.57 nM 8.18
CHEMBL5270335 IC50 = 8.0 nM 8.10
CHEMBL5284486 IC50 = 8.0 nM 8.10
CHEMBL5271640 IC50 = 9.0 nM 8.05
CHEMBL5273438 IC50 = 9.0 nM 8.05
CHEMBL5279491 IC50 = 9.8 nM 8.01
CHEMBL5271718 IC50 = 11.0 nM 7.96
CHEMBL5266834 IC50 = 11.0 nM 7.96
CHEMBL5284387 IC50 = 13.0 nM 7.89
CHEMBL5272345 IC50 = 14.0 nM 7.85
CHEMBL5284255 IC50 = 15.0 nM 7.82
CHEMBL5266482 IC50 = 22.0 nM 7.66
CHEMBL5281203 IC50 = 23.0 nM 7.64
CHEMBL3353404 IC50 = 32.0 nM 7.50
CHEMBL1173655 AFATINIB IC50 = 36.0 nM 7.44
CHEMBL5276760 IC50 = 37.6 nM 7.42
CHEMBL5291010 IC50 = 52.0 nM 7.28
CHEMBL5266896 IC50 = 53.0 nM 7.28
CHEMBL3353410 OSIMERTINIB IC50 = 53.0 nM 7.28
CHEMBL4104658 IC50 = 54.0 nM 7.27
CHEMBL3545308 ROCILETINIB IC50 = 179.0 nM 6.75
CHEMBL5286532 IC50 = 754.0 nM 6.12