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Assay Detail

CHEMBL734087

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Binding
Dissociation constant at Tm against human Mitogen-activated protein kinase p38 alpha (fluorescence exchange curve)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
Kroe RR, Regan J, Proto A, Peet GW, Roy T, Landro LD, Fuschetto NG, Pargellis CA, Ingraham RH.
J Med Chem (2003) 46 : 4669 -4675
PubMed 14561086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 8.36 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318810 1 10.05
CHEMBL103667 DORAMAPIMOD 2.0 1 10.00
CHEMBL143134 1 9.30
CHEMBL420047 1 9.00
CHEMBL105248 1 8.22
CHEMBL315100 1 7.68
CHEMBL104749 1 7.64
CHEMBL444613 1 7.44
CHEMBL87277 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318810 Kd = 0.09 nM 10.05
CHEMBL103667 DORAMAPIMOD Kd = 0.1 nM 10.00
CHEMBL143134 Kd = 0.5 nM 9.30
CHEMBL420047 Kd = 1.0 nM 9.00
CHEMBL105248 Kd = 6.0 nM 8.22
CHEMBL315100 Kd = 21.0 nM 7.68
CHEMBL104749 Kd = 23.0 nM 7.64
CHEMBL444613 Kd = 36.0 nM 7.44
CHEMBL87277 Kd = 1160.0 nM 5.94