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Assay Detail

CHEMBL4481536

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

Binding
Inhibition of N-terminal His-tagged MKK7 beta1 S273D/T275D double mutant (unknown origin) expressed in insect cells using JNK1 K55M mutant as substrate by ADP-Glo assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.
Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D.
J Med Chem (2019) 62 : 2843 -2848
PubMed 30768270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.88 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581088 1 8.00
CHEMBL4071151 1 7.40
CHEMBL1873475 IBRUTINIB 4.0 1 7.11
CHEMBL4094959 1 6.52
CHEMBL4584630 1 6.17
CHEMBL4534592 1 6.10
CHEMBL4588202 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581088 IC50 = 10.0 nM 8.00
CHEMBL4071151 IC50 = 40.0 nM 7.40
CHEMBL1873475 IBRUTINIB IC50 = 78.0 nM 7.11
CHEMBL4094959 IC50 = 302.0 nM 6.52
CHEMBL4584630 IC50 = 669.0 nM 6.17
CHEMBL4534592 IC50 = 788.0 nM 6.10
CHEMBL4588202 IC50 > 1000.0 nM -