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Assay Detail

CHEMBL5581446

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Functional
Antiproliferative activity against mouse BaF3 cells harboring EGFR C797S/L858R/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 9.81 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593035 — — 1 11.00
CHEMBL5592071 — — 1 10.82
CHEMBL5595676 — — 1 10.82
CHEMBL5592293 — — 1 10.77
CHEMBL5591001 — — 1 10.55
CHEMBL5592796 — — 1 10.54
CHEMBL5593178 — — 1 10.17
CHEMBL3545311 BRIGATINIB 4.0 1 10.15
CHEMBL5591039 — — 1 10.10
CHEMBL5593426 — — 1 10.09
CHEMBL5596002 — — 1 10.01
CHEMBL5595361 — — 1 9.99
CHEMBL5584002 — — 1 9.91
CHEMBL5583875 — — 1 9.76
CHEMBL5592057 — — 1 9.74
CHEMBL5593632 — — 1 9.73
CHEMBL5593280 — — 1 9.71
CHEMBL5595452 — — 1 9.68
CHEMBL5593247 — — 1 9.59
CHEMBL5593053 — — 1 9.55
CHEMBL5592255 — — 1 9.49
CHEMBL5593245 — — 1 9.45
CHEMBL5592376 — — 1 9.42
CHEMBL5595788 — — 1 9.40
CHEMBL5595484 — — 1 9.38
CHEMBL5595478 — — 1 9.21
CHEMBL5591186 — — 1 9.20
CHEMBL5594461 — — 1 9.16
CHEMBL5593051 — — 1 9.14
CHEMBL5593314 — — 1 9.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593035 — IC50 = 0.01 nM 11.00
CHEMBL5592071 — IC50 = 0.015 nM 10.82
CHEMBL5595676 — IC50 = 0.015 nM 10.82
CHEMBL5592293 — IC50 = 0.017 nM 10.77
CHEMBL5591001 — IC50 = 0.028 nM 10.55
CHEMBL5592796 — IC50 = 0.029 nM 10.54
CHEMBL5593178 — IC50 = 0.067 nM 10.17
CHEMBL3545311 BRIGATINIB IC50 = 0.071 nM 10.15
CHEMBL5591039 — IC50 = 0.079 nM 10.10
CHEMBL5593426 — IC50 = 0.082 nM 10.09
CHEMBL5596002 — IC50 = 0.098 nM 10.01
CHEMBL5595361 — IC50 = 0.103 nM 9.99
CHEMBL5584002 — IC50 = 0.124 nM 9.91
CHEMBL5583875 — IC50 = 0.175 nM 9.76
CHEMBL5592057 — IC50 = 0.183 nM 9.74
CHEMBL5593632 — IC50 = 0.185 nM 9.73
CHEMBL5593280 — IC50 = 0.196 nM 9.71
CHEMBL5595452 — IC50 = 0.211 nM 9.68
CHEMBL5593247 — IC50 = 0.257 nM 9.59
CHEMBL5593053 — IC50 = 0.284 nM 9.55
CHEMBL5592255 — IC50 = 0.324 nM 9.49
CHEMBL5593245 — IC50 = 0.356 nM 9.45
CHEMBL5592376 — IC50 = 0.377 nM 9.42
CHEMBL5595788 — IC50 = 0.398 nM 9.40
CHEMBL5595484 — IC50 = 0.413 nM 9.38
CHEMBL5595478 — IC50 = 0.613 nM 9.21
CHEMBL5591186 — IC50 = 0.631 nM 9.20
CHEMBL5594461 — IC50 = 0.698 nM 9.16
CHEMBL5593051 — IC50 = 0.723 nM 9.14
CHEMBL5593314 — IC50 = 0.785 nM 9.11
CHEMBL5594296 — IC50 = 0.791 nM 9.10
CHEMBL5594208 — IC50 = 0.844 nM 9.07
CHEMBL5590689 — IC50 = 0.001 nM -
CHEMBL5595208 — IC50 = 0.004 nM -
CHEMBL5584148 — IC50 = 0.003 nM -
CHEMBL5594833 — IC50 = 0.002 nM -
CHEMBL5590430 — IC50 = 0.004 nM -
CHEMBL5594458 — IC50 = 0.004 nM -