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Assay Detail

CHEMBL615267

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Binding
Inhibitory activity against inosine 5'-inosine monophosphate dehydrogenase type II (IMPDH II)
25
Total Activities
25
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

Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.
Chen P, Norris D, Haslow KD, Murali Dhar TG, Pitts WJ, Watterson SH, Cheney DL, Bassolino DA, Fleener CA, Rouleau KA, Hollenbaugh DL, Townsend RM, Barrish JC, Iwanowicz EJ.
Bioorg Med Chem Lett (2003) 13 : 1345 -1348
PubMed 12657279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.45 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280793 1 8.30
CHEMBL27948 1 7.75
CHEMBL285813 1 7.22
CHEMBL26741 1 6.82
CHEMBL29927 1 6.61
CHEMBL29926 1 6.40
CHEMBL27011 1 6.26
CHEMBL27529 1 6.13
CHEMBL26258 1 6.13
CHEMBL26155 1 6.09
CHEMBL416020 1 5.92
CHEMBL26419 1 5.78
CHEMBL282102 1 5.52
CHEMBL27528 1 5.42
CHEMBL285116 1 -
CHEMBL27189 1 -
CHEMBL282997 1 -
CHEMBL283016 1 -
CHEMBL26025 1 -
CHEMBL29480 1 -
CHEMBL28687 1 -
CHEMBL26259 1 -
CHEMBL285794 1 -
CHEMBL27753 1 -
CHEMBL284662 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280793 IC50 = 5.0 nM 8.30
CHEMBL27948 IC50 = 18.0 nM 7.75
CHEMBL285813 IC50 = 60.0 nM 7.22
CHEMBL26741 IC50 = 150.0 nM 6.82
CHEMBL29927 IC50 = 247.0 nM 6.61
CHEMBL29926 IC50 = 400.0 nM 6.40
CHEMBL27011 IC50 = 550.0 nM 6.26
CHEMBL27529 IC50 = 740.0 nM 6.13
CHEMBL26258 IC50 = 740.0 nM 6.13
CHEMBL26155 IC50 = 820.0 nM 6.09
CHEMBL416020 IC50 = 1200.0 nM 5.92
CHEMBL26419 IC50 = 1660.0 nM 5.78
CHEMBL282102 IC50 = 3000.0 nM 5.52
CHEMBL27528 IC50 = 3800.0 nM 5.42
CHEMBL285116 IC50 > 5000.0 nM -
CHEMBL27189 IC50 > 5000.0 nM -
CHEMBL282997 IC50 > 5000.0 nM -
CHEMBL283016 IC50 > 5000.0 nM -
CHEMBL26025 IC50 > 1700.0 nM -
CHEMBL29480 IC50 > 5000.0 nM -
CHEMBL28687 IC50 > 5000.0 nM -
CHEMBL26259 IC50 > 5000.0 nM -
CHEMBL285794 IC50 > 5000.0 nM -
CHEMBL27753 IC50 > 5000.0 nM -
CHEMBL284662 IC50 > 5000.0 nM -