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Assay Detail

CHEMBL1292995

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Binding
Inhibition of human IMPDH1 expressed in Escherichia coli strain BL21(DE3) after 60 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Inosine-5'-monophosphate dehydrogenase 1 (CHEMBL1822)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycophenolic acid derivatives.
Mitsuhashi S, Takenaka J, Iwamori K, Nakajima N, Ubukata M.
Bioorg Med Chem (2010) 18 : 8106 -8111
PubMed 20934342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.07 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL866 MYCOPHENOLIC ACID 4.0 1 7.72
CHEMBL132727 1 6.82
CHEMBL238461 MYCOPHENOLIC HYDROXAMIC ACID 1 6.46
CHEMBL157617 1 6.11
CHEMBL237760 1 5.82
CHEMBL238403 1 5.39
CHEMBL437376 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL866 MYCOPHENOLIC ACID IC50 = 19.0 nM 7.72
CHEMBL132727 IC50 = 150.0 nM 6.82
CHEMBL238461 MYCOPHENOLIC HYDROXAMIC ACID IC50 = 350.0 nM 6.46
CHEMBL157617 IC50 = 770.0 nM 6.11
CHEMBL237760 IC50 = 1500.0 nM 5.82
CHEMBL238403 IC50 = 4100.0 nM 5.39
CHEMBL437376 IC50 = 67000.0 nM 4.17