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Assay Detail

CHEMBL1781770

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

Binding
Inhibition of ALK assessed as biotin-EGPWLEEEEEAYGWMDF peptide phosphorylation by TR-FRET assay
21
Total Activities
21
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

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Kinoshita K, Ono Y, Emura T, Asoh K, Furuichi N, Ito T, Kawada H, Tanaka S, Morikami K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N.
Bioorg Med Chem Lett (2011) 21 : 3788 -3793
PubMed 21561771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.15 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779202 1 8.82
CHEMBL1779200 1 8.74
CHEMBL1779193 1 8.43
CHEMBL1779192 1 8.10
CHEMBL1779198 1 7.94
CHEMBL1779194 1 7.94
CHEMBL1779197 1 7.73
CHEMBL1779195 1 7.58
CHEMBL1779201 1 7.57
CHEMBL1779196 1 7.48
CHEMBL1779199 1 7.43
CHEMBL1779191 1 7.40
CHEMBL1779190 1 7.10
CHEMBL1779189 1 7.00
CHEMBL1779187 1 6.18
CHEMBL1779186 1 6.11
CHEMBL1779185 1 6.07
CHEMBL1779097 1 5.87
CHEMBL1779183 1 5.68
CHEMBL1779184 1 5.61
CHEMBL1779188 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779202 IC50 = 1.5 nM 8.82
CHEMBL1779200 IC50 = 1.8 nM 8.74
CHEMBL1779193 IC50 = 3.7 nM 8.43
CHEMBL1779192 IC50 = 8.0 nM 8.10
CHEMBL1779198 IC50 = 11.4 nM 7.94
CHEMBL1779194 IC50 = 11.6 nM 7.94
CHEMBL1779197 IC50 = 18.5 nM 7.73
CHEMBL1779195 IC50 = 26.2 nM 7.58
CHEMBL1779201 IC50 = 27.0 nM 7.57
CHEMBL1779196 IC50 = 33.4 nM 7.48
CHEMBL1779199 IC50 = 37.4 nM 7.43
CHEMBL1779191 IC50 = 40.0 nM 7.40
CHEMBL1779190 IC50 = 80.0 nM 7.10
CHEMBL1779189 IC50 = 100.0 nM 7.00
CHEMBL1779187 IC50 = 660.0 nM 6.18
CHEMBL1779186 IC50 = 770.0 nM 6.11
CHEMBL1779185 IC50 = 850.0 nM 6.07
CHEMBL1779097 IC50 = 1340.0 nM 5.87
CHEMBL1779183 IC50 = 2080.0 nM 5.68
CHEMBL1779184 IC50 = 2470.0 nM 5.61
CHEMBL1779188 IC50 = 3470.0 nM 5.46