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Assay Detail

CHEMBL2176367

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

Binding
Inhibition of ALK Tyr1604 phosphorylation by cell based assay
24
Total Activities
24
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

The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H, Epstein LF, Emkey R, Andrews PS, Yu VL, Saffran DC, Xu M, Drew A, Merkel P, Szilvassy S, Brake RL.
J Med Chem (2012) 55 : 6523 -6540
PubMed 22734674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.81 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172311 1 8.80
CHEMBL2172312 1 8.70
CHEMBL2172330 1 8.40
CHEMBL2172332 1 8.40
CHEMBL2172308 1 8.40
CHEMBL2172306 1 8.40
CHEMBL2172328 1 8.30
CHEMBL2172333 1 8.30
CHEMBL2172334 1 8.22
CHEMBL2172325 1 8.15
CHEMBL2172331 1 8.10
CHEMBL2172310 1 8.10
CHEMBL2172307 1 8.10
CHEMBL2172335 1 8.10
CHEMBL2172309 1 7.89
CHEMBL2172324 1 7.75
CHEMBL2172327 1 7.36
CHEMBL2172322 1 7.32
CHEMBL2172323 1 7.27
CHEMBL2172337 1 6.96
CHEMBL2172336 1 6.84
CHEMBL2172329 1 6.83
CHEMBL2172305 1 6.46
CHEMBL2172326 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172311 IC50 = 1.6 nM 8.80
CHEMBL2172312 IC50 = 2.0 nM 8.70
CHEMBL2172330 IC50 = 4.0 nM 8.40
CHEMBL2172332 IC50 = 4.0 nM 8.40
CHEMBL2172308 IC50 = 4.0 nM 8.40
CHEMBL2172306 IC50 = 4.0 nM 8.40
CHEMBL2172328 IC50 = 5.0 nM 8.30
CHEMBL2172333 IC50 = 5.0 nM 8.30
CHEMBL2172334 IC50 = 6.0 nM 8.22
CHEMBL2172325 IC50 = 7.0 nM 8.15
CHEMBL2172331 IC50 = 8.0 nM 8.10
CHEMBL2172310 IC50 = 8.0 nM 8.10
CHEMBL2172307 IC50 = 8.0 nM 8.10
CHEMBL2172335 IC50 = 8.0 nM 8.10
CHEMBL2172309 IC50 = 13.0 nM 7.89
CHEMBL2172324 IC50 = 18.0 nM 7.75
CHEMBL2172327 IC50 = 44.0 nM 7.36
CHEMBL2172322 IC50 = 48.0 nM 7.32
CHEMBL2172323 IC50 = 54.0 nM 7.27
CHEMBL2172337 IC50 = 109.0 nM 6.96
CHEMBL2172336 IC50 = 144.0 nM 6.84
CHEMBL2172329 IC50 = 147.0 nM 6.83
CHEMBL2172305 IC50 = 345.0 nM 6.46
CHEMBL2172326 IC50 = 562.0 nM 6.25