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Assay Detail

CHEMBL5581447

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Functional
Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/Del19/T790M mutant
ChEMBL ↗
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524) ↗
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation.
Yao H, Ren Y, Wu F, Liu J, Li J, Cao L, Yan M, Li X.
Eur J Med Chem (2024) 275 : 116590 -116590
PubMed 38908104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 9.78 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5592071 — — 1 10.96
CHEMBL5595676 — — 1 10.89
CHEMBL5592293 — — 1 10.82
CHEMBL5592796 — — 1 10.66
CHEMBL5591001 — — 1 10.62
CHEMBL5593178 — — 1 10.19
CHEMBL3545311 BRIGATINIB 4.0 1 10.19
CHEMBL5591039 — — 1 10.12
CHEMBL5593426 — — 1 10.10
CHEMBL5596002 — — 1 10.00
CHEMBL5595361 — — 1 9.94
CHEMBL5584002 — — 1 9.80
CHEMBL5592057 — — 1 9.75
CHEMBL5593280 — — 1 9.73
CHEMBL5583875 — — 1 9.72
CHEMBL5593632 — — 1 9.70
CHEMBL5595452 — — 1 9.70
CHEMBL5593247 — — 1 9.57
CHEMBL5593053 — — 1 9.56
CHEMBL5593245 — — 1 9.47
CHEMBL5592376 — — 1 9.46
CHEMBL5592255 — — 1 9.41
CHEMBL5595788 — — 1 9.39
CHEMBL5595484 — — 1 9.39
CHEMBL5595478 — — 1 9.22
CHEMBL5591186 — — 1 9.20
CHEMBL5594461 — — 1 9.17
CHEMBL5593051 — — 1 9.15
CHEMBL5594296 — — 1 9.11
CHEMBL5593314 — — 1 9.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5592071 — IC50 = 0.011 nM 10.96
CHEMBL5595676 — IC50 = 0.013 nM 10.89
CHEMBL5592293 — IC50 = 0.015 nM 10.82
CHEMBL5592796 — IC50 = 0.022 nM 10.66
CHEMBL5591001 — IC50 = 0.024 nM 10.62
CHEMBL5593178 — IC50 = 0.065 nM 10.19
CHEMBL3545311 BRIGATINIB IC50 = 0.065 nM 10.19
CHEMBL5591039 — IC50 = 0.075 nM 10.12
CHEMBL5593426 — IC50 = 0.079 nM 10.10
CHEMBL5596002 — IC50 = 0.101 nM 10.00
CHEMBL5595361 — IC50 = 0.115 nM 9.94
CHEMBL5584002 — IC50 = 0.159 nM 9.80
CHEMBL5592057 — IC50 = 0.177 nM 9.75
CHEMBL5593280 — IC50 = 0.185 nM 9.73
CHEMBL5583875 — IC50 = 0.191 nM 9.72
CHEMBL5593632 — IC50 = 0.198 nM 9.70
CHEMBL5595452 — IC50 = 0.199 nM 9.70
CHEMBL5593247 — IC50 = 0.271 nM 9.57
CHEMBL5593053 — IC50 = 0.274 nM 9.56
CHEMBL5593245 — IC50 = 0.342 nM 9.47
CHEMBL5592376 — IC50 = 0.351 nM 9.46
CHEMBL5592255 — IC50 = 0.388 nM 9.41
CHEMBL5595788 — IC50 = 0.41 nM 9.39
CHEMBL5595484 — IC50 = 0.407 nM 9.39
CHEMBL5595478 — IC50 = 0.608 nM 9.22
CHEMBL5591186 — IC50 = 0.635 nM 9.20
CHEMBL5594461 — IC50 = 0.682 nM 9.17
CHEMBL5593051 — IC50 = 0.712 nM 9.15
CHEMBL5593314 — IC50 = 0.769 nM 9.11
CHEMBL5594296 — IC50 = 0.775 nM 9.11
CHEMBL5594208 — IC50 = 0.795 nM 9.10
CHEMBL5590689 — IC50 = 0.001 nM -
CHEMBL5595208 — IC50 = 0.008 nM -
CHEMBL5584148 — IC50 = 0.004 nM -
CHEMBL5594833 — IC50 = 0.001 nM -
CHEMBL5590430 — IC50 = 0.003 nM -
CHEMBL5593035 — IC50 = 0.008 nM -
CHEMBL5594458 — IC50 = 0.004 nM -