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Assay Detail

CHEMBL4394511

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

ADMET
Cytotoxicity against human WS1 cells measured after 72 hrs by alamar blue assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
Asquith CRM, Naegeli KM, East MP, Laitinen T, Havener TM, Wells CI, Johnson GL, Drewry DH, Zuercher WJ, Morris DC.
J Med Chem (2019) 62 : 4772 -4778
PubMed 30973735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.89 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98248 1 5.54
CHEMBL304929 1 5.36
CHEMBL1092250 1 5.11
CHEMBL4447797 1 5.07
CHEMBL553 ERLOTINIB 4.0 1 5.07
CHEMBL29197 1 5.01
CHEMBL4443342 1 4.96
CHEMBL1089203 1 4.92
CHEMBL554 LAPATINIB 4.0 1 4.89
CHEMBL311959 1 4.85
CHEMBL111038 1 4.85
CHEMBL535429 1 4.68
CHEMBL939 GEFITINIB 4.0 1 4.64
CHEMBL309682 1 4.55
CHEMBL4446630 1 4.35
CHEMBL4518437 1 4.31
CHEMBL4468521 1 -
CHEMBL4440586 1 -
CHEMBL81073 1 -
CHEMBL4467033 1 -
CHEMBL4514780 1 -
CHEMBL4462395 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98248 IC50 = 2900.0 nM 5.54
CHEMBL304929 IC50 = 4400.0 nM 5.36
CHEMBL1092250 IC50 = 7700.0 nM 5.11
CHEMBL4447797 IC50 = 8600.0 nM 5.07
CHEMBL553 ERLOTINIB IC50 = 8600.0 nM 5.07
CHEMBL29197 IC50 = 9700.0 nM 5.01
CHEMBL4443342 IC50 = 11000.0 nM 4.96
CHEMBL1089203 IC50 = 12000.0 nM 4.92
CHEMBL554 LAPATINIB IC50 = 13000.0 nM 4.89
CHEMBL311959 IC50 = 14000.0 nM 4.85
CHEMBL111038 IC50 = 14000.0 nM 4.85
CHEMBL535429 IC50 = 21000.0 nM 4.68
CHEMBL939 GEFITINIB IC50 = 23000.0 nM 4.64
CHEMBL309682 IC50 = 28000.0 nM 4.55
CHEMBL4446630 IC50 = 45000.0 nM 4.35
CHEMBL4518437 IC50 = 49000.0 nM 4.31
CHEMBL4468521 IC50 > 50000.0 nM -
CHEMBL4440586 IC50 > 50000.0 nM -
CHEMBL81073 IC50 > 50000.0 nM -
CHEMBL4467033 IC50 > 10000.0 nM -
CHEMBL4514780 IC50 > 50000.0 nM -
CHEMBL4462395 IC50 > 50000.0 nM -