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Assay Detail

CHEMBL955774

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Binding
Inhibition of human MK2
17
Total Activities
17
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

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

Publication

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C.
Bioorg Med Chem Lett (2008) 18 : 6142 -6146
PubMed 18945615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.42 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516802 1 7.38
CHEMBL461139 1 7.29
CHEMBL461140 1 7.09
CHEMBL461316 1 6.82
CHEMBL507348 1 6.77
CHEMBL455156 1 6.72
CHEMBL516504 1 6.70
CHEMBL518824 1 6.54
CHEMBL460091 1 6.47
CHEMBL504267 1 6.46
CHEMBL455396 1 6.26
CHEMBL462579 1 5.91
CHEMBL462372 1 5.90
CHEMBL462578 1 5.89
CHEMBL452086 1 5.84
CHEMBL462371 1 5.77
CHEMBL452085 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516802 IC50 = 42.0 nM 7.38
CHEMBL461139 IC50 = 51.0 nM 7.29
CHEMBL461140 IC50 = 82.0 nM 7.09
CHEMBL461316 IC50 = 150.0 nM 6.82
CHEMBL507348 IC50 = 170.0 nM 6.77
CHEMBL455156 IC50 = 190.0 nM 6.72
CHEMBL516504 IC50 = 200.0 nM 6.70
CHEMBL518824 IC50 = 290.0 nM 6.54
CHEMBL460091 IC50 = 340.0 nM 6.47
CHEMBL504267 IC50 = 350.0 nM 6.46
CHEMBL455396 IC50 = 550.0 nM 6.26
CHEMBL462579 IC50 = 1230.0 nM 5.91
CHEMBL462372 IC50 = 1260.0 nM 5.90
CHEMBL462578 IC50 = 1300.0 nM 5.89
CHEMBL452086 IC50 = 1450.0 nM 5.84
CHEMBL462371 IC50 = 1700.0 nM 5.77
CHEMBL452085 IC50 = 5200.0 nM 5.28