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Assay Detail

CHEMBL699556

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

Binding
Inhibitory activity against inosine monophosphate dehydrogenase IMPDH II
36
Total Activities
34
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

Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.
Dhar TG, Watterson SH, Chen P, Shen Z, Gu HH, Norris D, Carlsen M, Haslow KD, Pitts WJ, Guo J, Chorba J, Fleener CA, Rouleau KA, Townsend R, Hollenbaugh D, Iwanowicz EJ.
Bioorg Med Chem Lett (2003) 13 : 547 -551
PubMed 12565969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.71 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153794 1 8.30
CHEMBL153118 1 8.22
CHEMBL422508 3 8.22
CHEMBL304087 MERIMEPODIB 2.0 1 8.00
CHEMBL423952 1 7.96
CHEMBL155617 1 7.92
CHEMBL357309 1 7.92
CHEMBL153389 1 7.89
CHEMBL866 MYCOPHENOLIC ACID 4.0 1 7.85
CHEMBL154752 1 7.85
CHEMBL357949 1 7.85
CHEMBL359344 1 7.82
CHEMBL357291 1 7.82
CHEMBL434894 1 7.82
CHEMBL149699 1 7.80
CHEMBL153516 1 7.75
CHEMBL154867 1 7.75
CHEMBL153411 1 7.70
CHEMBL153773 1 7.68
CHEMBL149755 1 7.68
CHEMBL153702 1 7.60
CHEMBL153429 1 7.58
CHEMBL153247 1 7.55
CHEMBL155616 1 7.52
CHEMBL153175 1 7.48
CHEMBL152978 1 7.28
CHEMBL150631 1 7.26
CHEMBL153595 1 7.17
CHEMBL153771 1 7.08
CHEMBL152931 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153794 IC50 = 5.0 nM 8.30
CHEMBL153118 IC50 = 6.0 nM 8.22
CHEMBL422508 IC50 = 6.0 nM 8.22
CHEMBL304087 MERIMEPODIB IC50 = 10.0 nM 8.00
CHEMBL423952 IC50 = 11.0 nM 7.96
CHEMBL155617 IC50 = 12.0 nM 7.92
CHEMBL357309 IC50 = 12.0 nM 7.92
CHEMBL153389 IC50 = 13.0 nM 7.89
CHEMBL357949 IC50 = 14.0 nM 7.85
CHEMBL154752 IC50 = 14.0 nM 7.85
CHEMBL866 MYCOPHENOLIC ACID IC50 = 14.0 nM 7.85
CHEMBL359344 IC50 = 15.0 nM 7.82
CHEMBL357291 IC50 = 15.0 nM 7.82
CHEMBL434894 IC50 = 15.0 nM 7.82
CHEMBL149699 IC50 = 16.0 nM 7.80
CHEMBL153516 IC50 = 18.0 nM 7.75
CHEMBL154867 IC50 = 18.0 nM 7.75
CHEMBL153411 IC50 = 20.0 nM 7.70
CHEMBL153773 IC50 = 21.0 nM 7.68
CHEMBL149755 IC50 = 21.0 nM 7.68
CHEMBL153702 IC50 = 25.0 nM 7.60
CHEMBL153429 IC50 = 26.0 nM 7.58
CHEMBL153247 IC50 = 28.0 nM 7.55
CHEMBL155616 IC50 = 30.0 nM 7.52
CHEMBL153175 IC50 = 33.0 nM 7.48
CHEMBL152978 IC50 = 53.0 nM 7.28
CHEMBL150631 IC50 = 55.0 nM 7.26
CHEMBL153595 IC50 = 68.0 nM 7.17
CHEMBL153771 IC50 = 83.0 nM 7.08
CHEMBL152931 IC50 = 140.0 nM 6.85
CHEMBL153481 IC50 < 5.0 nM -
CHEMBL151060 IC50 < 50.0 nM -
CHEMBL422508 IC50 < 5.0 nM -
CHEMBL422508 IC50 < 5.0 nM -
CHEMBL356881 IC50 < 5.0 nM -
CHEMBL356236 IC50 < 10.0 nM -