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Assay Detail

CHEMBL698781

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

Binding
Inhibition of human inosine monophosphate dehydrogenase IMPDH II
31
Total Activities
31
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

Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.
Watterson SH, Carlsen M, Dhar TG, Shen Z, Pitts WJ, Guo J, Gu HH, Norris D, Chorba J, Chen P, Cheney D, Witmer M, Fleener CA, Rouleau K, Townsend R, Hollenbaugh DL, Iwanowicz EJ.
Bioorg Med Chem Lett (2003) 13 : 543 -546
PubMed 12565968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.38 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152910 1 8.30
CHEMBL150777 1 8.30
CHEMBL23843 1 8.10
CHEMBL347721 1 8.05
CHEMBL866 MYCOPHENOLIC ACID 4.0 1 7.85
CHEMBL150728 1 7.75
CHEMBL65013 1 7.72
CHEMBL356371 1 7.72
CHEMBL153241 1 7.66
CHEMBL345992 1 7.54
CHEMBL153387 1 7.50
CHEMBL153032 1 7.47
CHEMBL153014 1 7.37
CHEMBL153511 1 7.37
CHEMBL151220 1 7.34
CHEMBL153223 1 7.20
CHEMBL153187 1 7.19
CHEMBL359340 1 7.19
CHEMBL424508 1 7.16
CHEMBL150487 1 6.96
CHEMBL151112 1 6.80
CHEMBL358383 1 6.80
CHEMBL153759 1 6.75
CHEMBL346396 1 6.70
CHEMBL357069 1 6.66
CHEMBL359161 1 6.52
CHEMBL149638 1 -
CHEMBL152959 1 -
CHEMBL358876 1 -
CHEMBL153715 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152910 IC50 = 5.0 nM 8.30
CHEMBL150777 IC50 = 5.0 nM 8.30
CHEMBL23843 IC50 = 8.0 nM 8.10
CHEMBL347721 IC50 = 9.0 nM 8.05
CHEMBL866 MYCOPHENOLIC ACID IC50 = 14.0 nM 7.85
CHEMBL150728 IC50 = 18.0 nM 7.75
CHEMBL65013 IC50 = 19.0 nM 7.72
CHEMBL356371 IC50 = 19.0 nM 7.72
CHEMBL153241 IC50 = 22.0 nM 7.66
CHEMBL345992 IC50 = 29.0 nM 7.54
CHEMBL153387 IC50 = 32.0 nM 7.50
CHEMBL153032 IC50 = 34.0 nM 7.47
CHEMBL153014 IC50 = 43.0 nM 7.37
CHEMBL153511 IC50 = 43.0 nM 7.37
CHEMBL151220 IC50 = 46.0 nM 7.34
CHEMBL153223 IC50 = 63.0 nM 7.20
CHEMBL153187 IC50 = 65.0 nM 7.19
CHEMBL359340 IC50 = 65.0 nM 7.19
CHEMBL424508 IC50 = 70.0 nM 7.16
CHEMBL150487 IC50 = 110.0 nM 6.96
CHEMBL151112 IC50 = 160.0 nM 6.80
CHEMBL358383 IC50 = 160.0 nM 6.80
CHEMBL153759 IC50 = 180.0 nM 6.75
CHEMBL346396 IC50 = 200.0 nM 6.70
CHEMBL357069 IC50 = 220.0 nM 6.66
CHEMBL359161 IC50 = 300.0 nM 6.52
CHEMBL149638 IC50 > 1000.0 nM -
CHEMBL152959 IC50 < 5.0 nM -
CHEMBL358876 IC50 < 5.0 nM -
CHEMBL153715 IC50 > 10000.0 nM -
CHEMBL152988 IC50 < 5.0 nM -