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Assay Detail

CHEMBL981158

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Binding
Inhibition of human IMP dehydrogenase 2
13
Total Activities
13
Compounds Tested
2
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 2 (CHEMBL2002)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bis(sulfonamide) isosters of mycophenolic adenine dinucleotide analogues: inhibition of inosine monophosphate dehydrogenase.
Chen L, Petrelli R, Olesiak M, Wilson DJ, Labello NP, Pankiewicz KW.
Bioorg Med Chem (2008) 16 : 7462 -7469
PubMed 18583139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.63 8.00
IC50 1 4.73 4.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL866 MYCOPHENOLIC ACID 4.0 1 8.00
CHEMBL392204 1 7.40
CHEMBL410745 1 6.96
CHEMBL446927 1 6.77
CHEMBL389392 1 6.75
CHEMBL410744 1 6.60
CHEMBL510826 1 6.51
CHEMBL444916 1 6.36
CHEMBL504308 1 5.52
CHEMBL476562 MYCOPHENOLIC BIS(SULFONAMIDE) 1 5.40
CHEMBL508103 1 4.73
CHEMBL477 ADENOSINE 4.0 1 -
CHEMBL476563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL866 MYCOPHENOLIC ACID Ki = 10.0 nM 8.00
CHEMBL392204 Ki = 40.0 nM 7.40
CHEMBL410745 Ki = 110.0 nM 6.96
CHEMBL446927 Ki = 170.0 nM 6.77
CHEMBL389392 Ki = 180.0 nM 6.75
CHEMBL410744 Ki = 250.0 nM 6.60
CHEMBL510826 Ki = 310.0 nM 6.51
CHEMBL444916 Ki = 440.0 nM 6.36
CHEMBL504308 Ki = 3000.0 nM 5.52
CHEMBL476562 MYCOPHENOLIC BIS(SULFONAMIDE) Ki = 4000.0 nM 5.40
CHEMBL508103 IC50 = 18800.0 nM 4.73
CHEMBL477 ADENOSINE Ki > 100000.0 nM -
CHEMBL476563 Ki > 100000.0 nM -