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Assay Detail

CHEMBL1648481

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Binding
Inhibition of ALK by cell based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

ALK tyrosine kinase receptor (CHEMBL4247)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Mesaros EF, Burke JP, Parrish JD, Dugan BJ, Anzalone AV, Angeles TS, Albom MS, Aimone LD, Quail MR, Wan W, Lu L, Huang Z, Ator MA, Ruggeri BA, Cheng M, Ott GR, Dorsey BD.
Bioorg Med Chem Lett (2011) 21 : 463 -466
PubMed 21074994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.14 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642258 1 7.52
CHEMBL1642263 1 7.40
CHEMBL1642265 1 7.40
CHEMBL458997 1 7.30
CHEMBL1642260 1 7.19
CHEMBL1642261 1 7.19
CHEMBL1642264 1 7.19
CHEMBL1642257 1 7.00
CHEMBL1642262 1 7.00
CHEMBL1642253 1 6.92
CHEMBL1642255 1 6.82
CHEMBL1642254 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642258 IC50 = 30.0 nM 7.52
CHEMBL1642263 IC50 = 40.0 nM 7.40
CHEMBL1642265 IC50 = 40.0 nM 7.40
CHEMBL458997 IC50 = 50.0 nM 7.30
CHEMBL1642260 IC50 = 65.0 nM 7.19
CHEMBL1642261 IC50 = 65.0 nM 7.19
CHEMBL1642264 IC50 = 65.0 nM 7.19
CHEMBL1642257 IC50 = 100.0 nM 7.00
CHEMBL1642262 IC50 = 100.0 nM 7.00
CHEMBL1642253 IC50 = 120.0 nM 6.92
CHEMBL1642255 IC50 = 150.0 nM 6.82
CHEMBL1642254 IC50 = 175.0 nM 6.76