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Assay Detail

CHEMBL4335546

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

Binding
Inhibition of MKK7 beta1 S273D/T275D double mutant (unknown origin) using JNK1 K55M mutant as substrate by ADP-Glo assay
20
Total Activities
20
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

Characterization of Covalent Pyrazolopyrimidine-MKK7 Complexes and a Report on a Unique DFG-in/Leu-in Conformation of Mitogen-Activated Protein Kinase Kinase 7 (MKK7).
Wolle P, Engel J, Smith S, Goebel L, Hennes E, Lategahn J, Rauh D.
J Med Chem (2019) 62 : 5541 -5546
PubMed 31083997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.73 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072299 1 8.07
CHEMBL4103201 1 7.72
CHEMBL4091966 1 7.46
CHEMBL1873475 IBRUTINIB 4.0 1 7.11
CHEMBL4090601 1 6.95
CHEMBL4095447 1 6.83
CHEMBL4062509 1 6.81
CHEMBL2180204 1 6.80
CHEMBL4094959 1 6.52
CHEMBL4099254 1 6.51
CHEMBL4099713 1 6.38
CHEMBL4094527 1 6.20
CHEMBL2180203 1 6.18
CHEMBL4082783 1 5.80
CHEMBL4101735 1 5.58
CHEMBL4081698 1 -
CHEMBL4103121 1 -
CHEMBL4083739 1 -
CHEMBL4463840 1 -
CHEMBL4452101 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072299 IC50 = 8.6 nM 8.07
CHEMBL4103201 IC50 = 19.0 nM 7.72
CHEMBL4091966 IC50 = 35.0 nM 7.46
CHEMBL1873475 IBRUTINIB IC50 = 78.0 nM 7.11
CHEMBL4090601 IC50 = 113.0 nM 6.95
CHEMBL4095447 IC50 = 149.0 nM 6.83
CHEMBL4062509 IC50 = 154.0 nM 6.81
CHEMBL2180204 IC50 = 159.0 nM 6.80
CHEMBL4094959 IC50 = 302.0 nM 6.52
CHEMBL4099254 IC50 = 307.0 nM 6.51
CHEMBL4099713 IC50 = 413.0 nM 6.38
CHEMBL4094527 IC50 = 631.0 nM 6.20
CHEMBL2180203 IC50 = 666.0 nM 6.18
CHEMBL4082783 IC50 = 1572.0 nM 5.80
CHEMBL4101735 IC50 = 2611.0 nM 5.58
CHEMBL4081698 IC50 > 10000.0 nM -
CHEMBL4103121 IC50 > 10000.0 nM -
CHEMBL4083739 IC50 > 10000.0 nM -
CHEMBL4463840 IC50 > 10000.0 nM -
CHEMBL4452101 IC50 > 10000.0 nM -