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Assay Detail

CHEMBL1050683

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

Binding
Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of JNK2 by enzyme fragment complementation assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Displacement assay for the detection of stabilizers of inactive kinase conformations.
Klüter S, Grütter C, Naqvi T, Rabiller M, Simard JR, Pawar V, Getlik M, Rauh D.
J Med Chem (2010) 53 : 357 -367
PubMed 19928858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.47 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103667 DORAMAPIMOD 2.0 1 7.57
CHEMBL522387 1 7.16
CHEMBL570904 1 7.00
CHEMBL585902 AMG-548 1.0 1 6.66
CHEMBL568875 1 6.36
CHEMBL497033 1 6.11
CHEMBL497615 1 5.92
CHEMBL101035 1 5.75
CHEMBL569943 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103667 DORAMAPIMOD IC50 = 27.0 nM 7.57
CHEMBL522387 IC50 = 70.0 nM 7.16
CHEMBL570904 IC50 = 100.0 nM 7.00
CHEMBL585902 AMG-548 IC50 = 220.0 nM 6.66
CHEMBL568875 IC50 = 440.0 nM 6.36
CHEMBL497033 IC50 = 770.0 nM 6.11
CHEMBL497615 IC50 = 1200.0 nM 5.92
CHEMBL101035 IC50 = 1800.0 nM 5.75
CHEMBL569943 IC50 = 1900.0 nM 5.72