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Assay Detail

CHEMBL1780728

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Binding
Inhibition of MK2 pretreated for 30 mins before substrate addition measured after 2 hrs by IMAP assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

MAP kinase-activated protein kinase 2 (CHEMBL2208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based lead identification of ATP-competitive MK2 inhibitors.
Barf T, Kaptein A, de Wilde S, van der Heijden R, van Someren R, Demont D, Schultz-Fademrecht C, Versteegh J, van Zeeland M, Seegers N, Kazemier B, van de Kar B, van Hoek M, de Roos J, Klop H, Smeets R, Hofstra C, Hornberg J, Oubrie A.
Bioorg Med Chem Lett (2011) 21 : 3818 -3822
PubMed 21565500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.49 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738702 1 8.40
CHEMBL1779361 1 8.22
CHEMBL1738780 1 7.55
CHEMBL226403 1 7.31
CHEMBL1779517 1 6.82
CHEMBL1779516 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738702 EC50 = 4.0 nM 8.40
CHEMBL1779361 EC50 = 6.0 nM 8.22
CHEMBL1738780 EC50 = 28.0 nM 7.55
CHEMBL226403 EC50 = 49.0 nM 7.31
CHEMBL1779517 EC50 = 151.0 nM 6.82
CHEMBL1779516 EC50 = 234.0 nM 6.63