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Assay Detail

CHEMBL5581448

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

Functional
Antiproliferative activity against human NCI-H1975 cells harboring EGFR double mutation
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1975
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1975 (CHEMBL614348)
Type CELL-LINE
Organism Homo sapiens

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 33 9.85 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5590430 1 10.89
CHEMBL5592293 1 10.62
CHEMBL5584148 1 10.59
CHEMBL5593035 1 10.46
CHEMBL5592071 1 10.38
CHEMBL5594458 1 10.36
CHEMBL5594833 1 10.20
CHEMBL5595676 1 10.14
CHEMBL5590689 1 10.13
CHEMBL5592255 1 10.08
CHEMBL5592796 1 10.06
CHEMBL5593632 1 10.02
CHEMBL5593245 1 9.98
CHEMBL5595208 1 9.97
CHEMBL5593053 1 9.96
CHEMBL5591001 1 9.91
CHEMBL5595361 1 9.90
CHEMBL5593247 1 9.82
CHEMBL5584002 1 9.78
CHEMBL5595788 1 9.71
CHEMBL5592376 1 9.70
CHEMBL5583875 1 9.63
CHEMBL5595484 1 9.63
CHEMBL5595478 1 9.57
CHEMBL5591186 1 9.54
CHEMBL5594461 1 9.53
CHEMBL5593314 1 9.45
CHEMBL5593051 1 9.40
CHEMBL5594208 1 9.26
CHEMBL5594296 1 9.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5590430 IC50 = 0.013 nM 10.89
CHEMBL5592293 IC50 = 0.024 nM 10.62
CHEMBL5584148 IC50 = 0.026 nM 10.59
CHEMBL5593035 IC50 = 0.035 nM 10.46
CHEMBL5592071 IC50 = 0.042 nM 10.38
CHEMBL5594458 IC50 = 0.044 nM 10.36
CHEMBL5594833 IC50 = 0.063 nM 10.20
CHEMBL5595676 IC50 = 0.072 nM 10.14
CHEMBL5590689 IC50 = 0.074 nM 10.13
CHEMBL5592255 IC50 = 0.084 nM 10.08
CHEMBL5592796 IC50 = 0.087 nM 10.06
CHEMBL5593632 IC50 = 0.095 nM 10.02
CHEMBL5593245 IC50 = 0.104 nM 9.98
CHEMBL5595208 IC50 = 0.106 nM 9.97
CHEMBL5593053 IC50 = 0.109 nM 9.96
CHEMBL5591001 IC50 = 0.123 nM 9.91
CHEMBL5595361 IC50 = 0.127 nM 9.90
CHEMBL5593247 IC50 = 0.152 nM 9.82
CHEMBL5584002 IC50 = 0.165 nM 9.78
CHEMBL5595788 IC50 = 0.195 nM 9.71
CHEMBL5592376 IC50 = 0.198 nM 9.70
CHEMBL5583875 IC50 = 0.236 nM 9.63
CHEMBL5595484 IC50 = 0.232 nM 9.63
CHEMBL5595478 IC50 = 0.266 nM 9.57
CHEMBL5591186 IC50 = 0.285 nM 9.54
CHEMBL5594461 IC50 = 0.295 nM 9.53
CHEMBL5593314 IC50 = 0.359 nM 9.45
CHEMBL5593051 IC50 = 0.394 nM 9.40
CHEMBL5594208 IC50 = 0.549 nM 9.26
CHEMBL5594296 IC50 = 0.642 nM 9.19
CHEMBL5593280 IC50 = 0.891 nM 9.05
CHEMBL5595452 IC50 = 0.915 nM 9.04
CHEMBL5592057 IC50 = 0.923 nM 9.04