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Assay Detail

CHEMBL5581449

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

Functional
Antiproliferative activity against human PC-9 cells harboring EGFR single mutation
ChEMBL ↗
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-9
Confidence 1 — Organism
Curated By Autocuration

Target

PC-9 (CHEMBL614102) ↗
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 10.16 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593632 — — 1 10.96
CHEMBL5594833 — — 1 10.74
CHEMBL5590430 — — 1 10.72
CHEMBL5593035 — — 1 10.68
CHEMBL5592071 — — 1 10.52
CHEMBL5584148 — — 1 10.51
CHEMBL5594458 — — 1 10.48
CHEMBL5593053 — — 1 10.41
CHEMBL5592255 — — 1 10.35
CHEMBL5590689 — — 1 10.35
CHEMBL5592293 — — 1 10.33
CHEMBL5592796 — — 1 10.29
CHEMBL5595208 — — 1 10.28
CHEMBL5595361 — — 1 10.24
CHEMBL5591001 — — 1 10.21
CHEMBL5595676 — — 1 10.12
CHEMBL5593245 — — 1 10.12
CHEMBL5595478 — — 1 10.07
CHEMBL5584002 — — 1 10.05
CHEMBL5593314 — — 1 10.03
CHEMBL5595452 — — 1 9.98
CHEMBL5593051 — — 1 9.97
CHEMBL5594208 — — 1 9.94
CHEMBL5593280 — — 1 9.91
CHEMBL5583875 — — 1 9.87
CHEMBL5592376 — — 1 9.86
CHEMBL5592057 — — 1 9.85
CHEMBL5594461 — — 1 9.84
CHEMBL5594296 — — 1 9.81
CHEMBL5595788 — — 1 9.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593632 — IC50 = 0.011 nM 10.96
CHEMBL5594833 — IC50 = 0.018 nM 10.74
CHEMBL5590430 — IC50 = 0.019 nM 10.72
CHEMBL5593035 — IC50 = 0.021 nM 10.68
CHEMBL5592071 — IC50 = 0.03 nM 10.52
CHEMBL5584148 — IC50 = 0.031 nM 10.51
CHEMBL5594458 — IC50 = 0.033 nM 10.48
CHEMBL5593053 — IC50 = 0.039 nM 10.41
CHEMBL5592255 — IC50 = 0.045 nM 10.35
CHEMBL5590689 — IC50 = 0.045 nM 10.35
CHEMBL5592293 — IC50 = 0.047 nM 10.33
CHEMBL5592796 — IC50 = 0.051 nM 10.29
CHEMBL5595208 — IC50 = 0.052 nM 10.28
CHEMBL5595361 — IC50 = 0.057 nM 10.24
CHEMBL5591001 — IC50 = 0.061 nM 10.21
CHEMBL5593245 — IC50 = 0.075 nM 10.12
CHEMBL5595676 — IC50 = 0.075 nM 10.12
CHEMBL5595478 — IC50 = 0.085 nM 10.07
CHEMBL5584002 — IC50 = 0.089 nM 10.05
CHEMBL5593314 — IC50 = 0.094 nM 10.03
CHEMBL5595452 — IC50 = 0.105 nM 9.98
CHEMBL5593051 — IC50 = 0.106 nM 9.97
CHEMBL5594208 — IC50 = 0.116 nM 9.94
CHEMBL5593280 — IC50 = 0.123 nM 9.91
CHEMBL5583875 — IC50 = 0.134 nM 9.87
CHEMBL5592376 — IC50 = 0.138 nM 9.86
CHEMBL5592057 — IC50 = 0.143 nM 9.85
CHEMBL5594461 — IC50 = 0.144 nM 9.84
CHEMBL5594296 — IC50 = 0.154 nM 9.81
CHEMBL5595788 — IC50 = 0.158 nM 9.80
CHEMBL5595484 — IC50 = 0.177 nM 9.75
CHEMBL5593247 — IC50 = 0.215 nM 9.67
CHEMBL5591186 — IC50 = 0.267 nM 9.57