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Assay Detail

CHEMBL4255097

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

Binding
Inhibition of recombinant full length human ASK1 expressed in HEK293/AP1-Luc cells assessed as reduction in p38 phosphorylation after 18 hrs by HTRF assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 5 (CHEMBL5285)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW.
Eur J Med Chem (2018) 145 : 606 -621
PubMed 29348070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.97 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4294318 1 7.55
CHEMBL4290518 1 7.39
CHEMBL4289040 1 7.14
CHEMBL4283739 1 7.08
CHEMBL4282644 1 7.03
CHEMBL4287097 1 6.85
CHEMBL4279174 1 6.57
CHEMBL4278211 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4294318 IC50 = 28.0 nM 7.55
CHEMBL4290518 IC50 = 41.0 nM 7.39
CHEMBL4289040 IC50 = 73.0 nM 7.14
CHEMBL4283739 IC50 = 84.0 nM 7.08
CHEMBL4282644 IC50 = 94.0 nM 7.03
CHEMBL4287097 IC50 = 140.0 nM 6.85
CHEMBL4279174 IC50 = 272.0 nM 6.57
CHEMBL4278211 IC50 = 736.0 nM 6.13