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Assay Detail

CHEMBL866272

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Binding
Inhibition of IMPDH2
24
Total Activities
24
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

Inosine-5'-monophosphate dehydrogenase 2 (CHEMBL2002)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships.
Beevers RE, Buckley GM, Davies N, Fraser JL, Galvin FC, Hannah DR, Haughan AF, Jenkins K, Mack SR, Pitt WR, Ratcliffe AJ, Richard MD, Sabin V, Sharpe A, Williams SC.
Bioorg Med Chem Lett (2006) 16 : 2539 -2542
PubMed 16483773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.61 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380639 1 7.12
CHEMBL206886 1 7.08
CHEMBL208219 1 6.89
CHEMBL379524 1 6.65
CHEMBL380132 1 6.44
CHEMBL207621 1 6.34
CHEMBL208261 1 6.23
CHEMBL333482 1 6.14
CHEMBL205218 1 5.96
CHEMBL380071 1 5.94
CHEMBL426498 1 5.93
CHEMBL205051 1 5.87
CHEMBL378169 1 5.39
CHEMBL377529 1 5.21
CHEMBL205035 1 5.12
CHEMBL205236 1 5.12
CHEMBL379401 1 5.11
CHEMBL205328 1 4.81
CHEMBL208524 1 4.77
CHEMBL207730 1 4.71
CHEMBL378273 1 4.68
CHEMBL46724 1 4.68
CHEMBL206945 1 4.23
CHEMBL377680 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380639 IC50 = 76.0 nM 7.12
CHEMBL206886 IC50 = 84.0 nM 7.08
CHEMBL208219 IC50 = 128.0 nM 6.89
CHEMBL379524 IC50 = 222.0 nM 6.65
CHEMBL380132 IC50 = 364.0 nM 6.44
CHEMBL207621 IC50 = 456.0 nM 6.34
CHEMBL208261 IC50 = 586.0 nM 6.23
CHEMBL333482 IC50 = 722.0 nM 6.14
CHEMBL205218 IC50 = 1110.0 nM 5.96
CHEMBL380071 IC50 = 1150.0 nM 5.94
CHEMBL426498 IC50 = 1170.0 nM 5.93
CHEMBL205051 IC50 = 1360.0 nM 5.87
CHEMBL378169 IC50 = 4040.0 nM 5.39
CHEMBL377529 IC50 = 6210.0 nM 5.21
CHEMBL205035 IC50 = 7660.0 nM 5.12
CHEMBL205236 IC50 = 7680.0 nM 5.12
CHEMBL379401 IC50 = 7850.0 nM 5.11
CHEMBL205328 IC50 = 15400.0 nM 4.81
CHEMBL208524 IC50 = 17000.0 nM 4.77
CHEMBL207730 IC50 = 19500.0 nM 4.71
CHEMBL378273 IC50 = 21000.0 nM 4.68
CHEMBL46724 IC50 = 20900.0 nM 4.68
CHEMBL206945 IC50 = 58400.0 nM 4.23
CHEMBL377680 IC50 = 71800.0 nM 4.14