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Assay Detail

CHEMBL697550

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human inosine-5'-monophosphate dehydrogenase 2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.
Dhar TG, Shen Z, Guo J, Liu C, Watterson SH, Gu HH, Pitts WJ, Fleener CA, Rouleau KA, Sherbina NZ, McIntyre KW, Shuster DJ, Witmer MR, Tredup JA, Chen BC, Zhao R, Bednarz MS, Cheney DL, MacMaster JF, Miller LM, Berry KK, Harper TW, Barrish JC, Hollenbaugh DL, Iwanowicz EJ.
J Med Chem (2002) 45 : 2127 -2130
PubMed 12014950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.51 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304087 MERIMEPODIB 2.0 1 8.00
CHEMBL68075 1 7.96
CHEMBL64830 1 7.92
CHEMBL67036 1 7.89
CHEMBL66614 1 7.89
CHEMBL866 MYCOPHENOLIC ACID 4.0 1 7.85
CHEMBL63158 1 7.82
CHEMBL302967 1 7.77
CHEMBL306453 1 7.75
CHEMBL64639 1 7.70
CHEMBL417047 1 7.70
CHEMBL305977 1 7.66
CHEMBL302748 1 7.64
CHEMBL67346 1 7.60
CHEMBL261978 1 7.57
CHEMBL65826 1 7.52
CHEMBL67794 1 7.16
CHEMBL302558 1 7.07
CHEMBL65962 1 7.07
CHEMBL430981 1 7.01
CHEMBL305786 1 6.98
CHEMBL66012 1 6.94
CHEMBL307084 1 6.90
CHEMBL66564 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304087 MERIMEPODIB IC50 = 10.0 nM 8.00
CHEMBL68075 IC50 = 11.0 nM 7.96
CHEMBL64830 IC50 = 12.0 nM 7.92
CHEMBL67036 IC50 = 13.0 nM 7.89
CHEMBL66614 IC50 = 13.0 nM 7.89
CHEMBL866 MYCOPHENOLIC ACID IC50 = 14.0 nM 7.85
CHEMBL63158 IC50 = 15.0 nM 7.82
CHEMBL302967 IC50 = 17.0 nM 7.77
CHEMBL306453 IC50 = 18.0 nM 7.75
CHEMBL64639 IC50 = 20.0 nM 7.70
CHEMBL417047 IC50 = 20.0 nM 7.70
CHEMBL305977 IC50 = 22.0 nM 7.66
CHEMBL302748 IC50 = 23.0 nM 7.64
CHEMBL67346 IC50 = 25.0 nM 7.60
CHEMBL261978 IC50 = 27.0 nM 7.57
CHEMBL65826 IC50 = 30.0 nM 7.52
CHEMBL67794 IC50 = 70.0 nM 7.16
CHEMBL302558 IC50 = 85.0 nM 7.07
CHEMBL65962 IC50 = 86.0 nM 7.07
CHEMBL430981 IC50 = 97.0 nM 7.01
CHEMBL305786 IC50 = 104.0 nM 6.98
CHEMBL66012 IC50 = 115.0 nM 6.94
CHEMBL307084 IC50 = 127.0 nM 6.90
CHEMBL66564 IC50 = 141.0 nM 6.85