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Assay Detail

CHEMBL1072653

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Binding
Inhibition of MK2
26
Total Activities
26
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

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV.
Bioorg Med Chem Lett (2010) 20 : 334 -337
PubMed 19926477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.19 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL590109 1 7.72
CHEMBL594090 1 7.70
CHEMBL592030 1 7.46
CHEMBL590612 1 7.43
CHEMBL603322 1 7.39
CHEMBL591797 1 7.25
CHEMBL600081 1 6.80
CHEMBL592288 1 6.80
CHEMBL591329 1 6.58
CHEMBL590834 1 6.51
CHEMBL595933 1 6.31
CHEMBL589650 1 6.14
CHEMBL591783 1 6.09
CHEMBL592031 1 6.02
CHEMBL590110 1 5.89
CHEMBL591071 1 5.85
CHEMBL591305 1 5.80
CHEMBL589853 1 5.72
CHEMBL596588 1 5.72
CHEMBL589626 1 5.47
CHEMBL591328 1 5.27
CHEMBL585958 1 5.04
CHEMBL584617 1 4.85
CHEMBL584423 1 4.62
CHEMBL584640 1 4.31
CHEMBL605922 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL590109 IC50 = 19.0 nM 7.72
CHEMBL594090 IC50 = 20.0 nM 7.70
CHEMBL592030 IC50 = 35.0 nM 7.46
CHEMBL590612 IC50 = 37.0 nM 7.43
CHEMBL603322 IC50 = 41.0 nM 7.39
CHEMBL591797 IC50 = 56.0 nM 7.25
CHEMBL600081 IC50 = 160.0 nM 6.80
CHEMBL592288 IC50 = 160.0 nM 6.80
CHEMBL591329 IC50 = 260.0 nM 6.58
CHEMBL590834 IC50 = 310.0 nM 6.51
CHEMBL595933 IC50 = 490.0 nM 6.31
CHEMBL589650 IC50 = 720.0 nM 6.14
CHEMBL591783 IC50 = 820.0 nM 6.09
CHEMBL592031 IC50 = 960.0 nM 6.02
CHEMBL590110 IC50 = 1300.0 nM 5.89
CHEMBL591071 IC50 = 1400.0 nM 5.85
CHEMBL591305 IC50 = 1600.0 nM 5.80
CHEMBL589853 IC50 = 1900.0 nM 5.72
CHEMBL596588 IC50 = 1900.0 nM 5.72
CHEMBL589626 IC50 = 3400.0 nM 5.47
CHEMBL591328 IC50 = 5400.0 nM 5.27
CHEMBL585958 IC50 = 9100.0 nM 5.04
CHEMBL584617 IC50 = 14000.0 nM 4.85
CHEMBL584423 IC50 = 24000.0 nM 4.62
CHEMBL584640 IC50 = 49000.0 nM 4.31
CHEMBL605922 IC50 > 50000.0 nM -