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Assay Detail

CHEMBL5120433

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

Functional
Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay
ChEMBL ↗
48
Total Activities
24
Compounds Tested
2
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 Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S, Rueher D, Imhoff MP, Raschetti N, Marty HP, Dietzig A, Rynn C, Ehler A, Burger D, Kornacker M, Schaffland JP, Herting F, Pao W, Bischoff JR, Martoglio B, Alice Nagel Y, Jaeschke G.
J Med Chem (2022) 65 : 13052 -13073
PubMed 36178776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.42 9.00
IC90 24 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5183324 — — 2 9.00
CHEMBL5177023 — — 2 8.70
CHEMBL5184760 — — 2 8.70
CHEMBL5189574 — — 2 8.70
CHEMBL5170519 — — 2 8.52
CHEMBL5184539 — — 2 8.40
CHEMBL5193594 — — 2 8.40
CHEMBL5208056 — — 2 7.92
CHEMBL5202945 — — 2 7.82
CHEMBL5180839 — — 2 7.80
CHEMBL5203543 — — 2 7.58
CHEMBL5207152 — — 2 7.44
CHEMBL5201725 — — 2 7.34
CHEMBL5207479 — — 2 7.14
CHEMBL5172668 — — 2 6.68
CHEMBL5180289 — — 2 6.19
CHEMBL5193772 — — 2 6.10
CHEMBL5187250 — — 2 5.90
CHEMBL5198433 — — 2 5.89
CHEMBL4443062 — — 2 5.81
CHEMBL5189114 — — 2 5.75
CHEMBL5170278 — — 2 -
CHEMBL5171139 — — 2 -
CHEMBL5173986 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5183324 — IC50 = 1.0 nM 9.00
CHEMBL5177023 — IC50 = 2.0 nM 8.70
CHEMBL5189574 — IC50 = 2.0 nM 8.70
CHEMBL5184760 — IC50 = 2.0 nM 8.70
CHEMBL5170519 — IC50 = 3.0 nM 8.52
CHEMBL5193594 — IC50 = 4.0 nM 8.40
CHEMBL5184539 — IC50 = 4.0 nM 8.40
CHEMBL5208056 — IC50 = 12.0 nM 7.92
CHEMBL5202945 — IC50 = 15.0 nM 7.82
CHEMBL5180839 — IC50 = 16.0 nM 7.80
CHEMBL5203543 — IC50 = 26.0 nM 7.58
CHEMBL5207152 — IC50 = 36.0 nM 7.44
CHEMBL5201725 — IC50 = 46.0 nM 7.34
CHEMBL5207479 — IC50 = 72.0 nM 7.14
CHEMBL5172668 — IC50 = 207.0 nM 6.68
CHEMBL5180289 — IC50 = 650.0 nM 6.19
CHEMBL5193772 — IC50 = 800.0 nM 6.10
CHEMBL5187250 — IC50 = 1250.0 nM 5.90
CHEMBL5198433 — IC50 = 1300.0 nM 5.89
CHEMBL4443062 — IC50 = 1550.0 nM 5.81
CHEMBL5189114 — IC50 = 1800.0 nM 5.75
CHEMBL5171139 — IC50 > 10000.0 nM -
CHEMBL5170278 — IC50 > 10000.0 nM -
CHEMBL5173986 — IC50 > 10000.0 nM -
CHEMBL5171139 — IC90 > 10000.0 nM -
CHEMBL5189114 — IC90 = 7000.0 nM -
CHEMBL5170278 — IC90 > 10000.0 nM -
CHEMBL5198433 — IC90 = 3100.0 nM -
CHEMBL5172668 — IC90 = 711.0 nM -
CHEMBL5187250 — IC90 = 3250.0 nM -
CHEMBL5207479 — IC90 = 285.0 nM -
CHEMBL5180839 — IC90 = 47.0 nM -
CHEMBL5189574 — IC90 = 5.0 nM -
CHEMBL5184539 — IC90 = 12.0 nM -
CHEMBL4443062 — IC90 = 7280.0 nM -
CHEMBL5177023 — IC90 = 2.0 nM -
CHEMBL5184760 — IC90 = 5.0 nM -
CHEMBL5193772 — IC90 = 2800.0 nM -
CHEMBL5170519 — IC90 = 8.0 nM -
CHEMBL5193594 — IC90 = 10.0 nM -
CHEMBL5208056 — IC90 = 32.0 nM -
CHEMBL5173986 — IC90 > 10000.0 nM -
CHEMBL5180289 — IC90 = 2600.0 nM -
CHEMBL5203543 — IC90 = 70.0 nM -
CHEMBL5183324 — IC90 = 2.0 nM -
CHEMBL5207152 — IC90 = 104.0 nM -
CHEMBL5202945 — IC90 = 42.0 nM -
CHEMBL5201725 — IC90 = 126.0 nM -