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Assay Detail

CHEMBL5511552

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

Binding
Inhibition of EGFR D770_N771insSVD mutant (unknown origin) phosphorylation transfected in human NCI-H2073 cells incubated for 2 hrs by HTRF assay
ChEMBL ↗
61
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H2073
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Barton P, Braybrooke E, Colclough N, Dong Z, Evans L, Floc'h N, Guérot C, Hargreaves D, Khurana P, Li S, Li X, Lister A, McCoull W, McWilliams L, Orme JP, Packer MJ, Swaih AM, Ward RA, Winlow P, Ye Y.
J Med Chem (2024) 67 : 8988 -9027
PubMed 38770784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 6.77 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4650281 CLN-081 3.0 2 7.68
CHEMBL5563485 — — 2 7.54
CHEMBL5561612 — — 2 7.54
CHEMBL5560320 — — 2 7.48
CHEMBL4650319 MOBOCERTINIB 4.0 2 7.47
CHEMBL5559367 — — 2 7.36
CHEMBL5568213 — — 2 7.15
CHEMBL5568516 — — 2 7.09
CHEMBL5567814 — — 2 7.09
CHEMBL5542205 — — 2 7.05
CHEMBL5560466 — — 2 7.05
CHEMBL5558799 — — 2 7.03
CHEMBL5556861 — — 2 7.01
CHEMBL5512556 — — 2 7.00
CHEMBL5537023 — — 2 6.92
CHEMBL5559071 — — 2 6.89
CHEMBL5555813 — — 2 6.77
CHEMBL5567575 — — 2 6.72
CHEMBL5559069 — — 2 6.68
CHEMBL5558098 — — 2 6.66
CHEMBL5517918 — — 2 6.64
CHEMBL5517919 — — 2 6.60
CHEMBL5512543 — — 2 6.58
CHEMBL5560711 — — 2 6.54
CHEMBL5523462 — — 2 6.27
CHEMBL5567954 — — 2 6.06
CHEMBL5563422 — — 2 6.00
CHEMBL5568120 — — 2 5.54
CHEMBL5562889 — — 2 5.48
CHEMBL5566816 — — 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4650281 CLN-081 IC50 = 21.0 nM 7.68
CHEMBL5563485 — IC50 = 29.0 nM 7.54
CHEMBL5561612 — IC50 = 29.0 nM 7.54
CHEMBL5560320 — IC50 = 33.0 nM 7.48
CHEMBL4650319 MOBOCERTINIB IC50 = 34.0 nM 7.47
CHEMBL5559367 — IC50 = 44.0 nM 7.36
CHEMBL5568213 — IC50 = 71.0 nM 7.15
CHEMBL5568516 — IC50 = 81.0 nM 7.09
CHEMBL5567814 — IC50 = 82.0 nM 7.09
CHEMBL5542205 — IC50 = 89.0 nM 7.05
CHEMBL5560466 — IC50 = 90.0 nM 7.05
CHEMBL5558799 — IC50 = 93.0 nM 7.03
CHEMBL5556861 — IC50 = 98.0 nM 7.01
CHEMBL5512556 — IC50 = 100.0 nM 7.00
CHEMBL5537023 — IC50 = 120.0 nM 6.92
CHEMBL5559071 — IC50 = 130.0 nM 6.89
CHEMBL5555813 — IC50 = 170.0 nM 6.77
CHEMBL5567575 — IC50 = 190.0 nM 6.72
CHEMBL5559069 — IC50 = 210.0 nM 6.68
CHEMBL5558098 — IC50 = 220.0 nM 6.66
CHEMBL5517918 — IC50 = 230.0 nM 6.64
CHEMBL5517919 — IC50 = 250.0 nM 6.60
CHEMBL5512543 — IC50 = 260.0 nM 6.58
CHEMBL5560711 — IC50 = 290.0 nM 6.54
CHEMBL5523462 — IC50 = 540.0 nM 6.27
CHEMBL5567954 — IC50 = 870.0 nM 6.06
CHEMBL5563422 — IC50 = 1000.0 nM 6.00
CHEMBL5568120 — IC50 = 2900.0 nM 5.54
CHEMBL5562889 — IC50 = 3300.0 nM 5.48
CHEMBL5566816 — IC50 = 5500.0 nM 5.26
CHEMBL5523462 — IC50 > 724435960.07 nM -
CHEMBL5567814 — IC50 > 724435960.07 nM -
CHEMBL5568213 — IC50 > 724435960.07 nM -
CHEMBL5517918 — IC50 > 724435960.07 nM -
CHEMBL5555813 — IC50 > 794328234.72 nM -
CHEMBL5556861 — IC50 > 831763771.1 nM -
CHEMBL5560466 — IC50 > 794328234.72 nM -
CHEMBL5568516 — IC50 > 794328234.72 nM -
CHEMBL5568120 — IC50 > 794328234.72 nM -
CHEMBL5560320 — IC50 > 794328234.72 nM -
CHEMBL5563485 — IC50 > 794328234.72 nM -
CHEMBL5559069 — IC50 > 831763771.1 nM -
CHEMBL5560711 — IC50 > 794328234.72 nM -
CHEMBL5558098 — IC50 > 831763771.1 nM -
CHEMBL5512543 — IC50 > 831763771.1 nM -
CHEMBL5542205 — IC50 > 870963589.96 nM -
CHEMBL5537023 — IC50 > 831763771.1 nM -
CHEMBL5559071 — IC50 > 831763771.1 nM -
CHEMBL4650319 MOBOCERTINIB IC50 > 870963589.96 nM -
CHEMBL4650281 CLN-081 IC50 > 870963589.96 nM -