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Assay Detail

CHEMBL5044556

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

Binding
Binding affinity to wild-type human full length p38-alpha (M1 to S360 residues) expressed in bacterial expression system by Kinomescan method
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 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
Cui H, Divakaran A, Hoell ZJ, Ellingson MO, Scholtz CR, Zahid H, Johnson JA, Griffith EC, Gee CT, Lee AL, Khanal S, Shi K, Aihara H, Shah VH, Lee RE, Harki DA, Pomerantz WCK.
J Med Chem (2022) 65 : 2342 -2360
PubMed 35007061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 6.87 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4521096 1 9.33
CHEMBL417255 1 7.39
CHEMBL5087797 1 7.01
CHEMBL5085236 1 7.00
CHEMBL5085763 1 6.58
CHEMBL5082732 1 6.11
CHEMBL5088918 1 5.82
CHEMBL5080097 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4521096 Kd = 0.47 nM 9.33
CHEMBL417255 Kd = 41.0 nM 7.39
CHEMBL5087797 Kd = 98.0 nM 7.01
CHEMBL5085236 Kd = 100.0 nM 7.00
CHEMBL5085763 Kd = 260.0 nM 6.58
CHEMBL5082732 Kd = 780.0 nM 6.11
CHEMBL5088918 Kd = 1500.0 nM 5.82
CHEMBL5080097 Kd = 1900.0 nM 5.72