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Assay Detail

CHEMBL669212

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Binding
Inhibitory activity against human liver Dihydrodipicolinate reductase (DHPR)
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Dihydropteridine reductase (CHEMBL3730)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and dihydropteridine reductase inhibitory effects of potential metabolites of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine.
Gessner W, Brossi A, Shen R, Abell CW.
J Med Chem (1985) 28 : 311 -317
PubMed 3871859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.31 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324880 1 6.55
CHEMBL110377 1 6.42
CHEMBL109090 1 6.20
CHEMBL108967 1 5.52
CHEMBL323998 1 5.47
CHEMBL105897 1 5.44
CHEMBL110621 1 5.30
CHEMBL108679 1 5.28
CHEMBL108787 1 5.23
CHEMBL108496 1 5.14
CHEMBL322323 1 5.03
CHEMBL109076 1 4.72
CHEMBL108680 1 4.57
CHEMBL321432 1 4.38
CHEMBL110602 1 4.36
CHEMBL109074 1 -
CHEMBL105891 1 -
CHEMBL101664 1 -
CHEMBL98417 1 -
CHEMBL6224 1 -
CHEMBL108926 1 -
CHEMBL108466 1 -
CHEMBL24172 1 -
CHEMBL106131 1 -
CHEMBL110142 1 -
CHEMBL440702 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324880 IC50 = 280.0 nM 6.55
CHEMBL110377 IC50 = 380.0 nM 6.42
CHEMBL109090 IC50 = 630.0 nM 6.20
CHEMBL108967 IC50 = 3000.0 nM 5.52
CHEMBL323998 IC50 = 3400.0 nM 5.47
CHEMBL105897 IC50 = 3600.0 nM 5.44
CHEMBL110621 IC50 = 5000.0 nM 5.30
CHEMBL108679 IC50 = 5200.0 nM 5.28
CHEMBL108787 IC50 = 5900.0 nM 5.23
CHEMBL108496 IC50 = 7200.0 nM 5.14
CHEMBL322323 IC50 = 9300.0 nM 5.03
CHEMBL109076 IC50 = 19000.0 nM 4.72
CHEMBL108680 IC50 = 27000.0 nM 4.57
CHEMBL321432 IC50 = 42000.0 nM 4.38
CHEMBL110602 IC50 = 44000.0 nM 4.36
CHEMBL109074 IC50 = 2400000.0 nM -
CHEMBL105891 IC50 = 5600000.0 nM -
CHEMBL101664 IC50 = 3400000.0 nM -
CHEMBL98417 IC50 = 23000000.0 nM -
CHEMBL6224 IC50 = 12000000.0 nM -
CHEMBL108926 IC50 = 10000000.0 nM -
CHEMBL108466 IC50 = 1100000.0 nM -
CHEMBL24172 IC50 = 3000000.0 nM -
CHEMBL106131 IC50 = 9400000.0 nM -
CHEMBL110142 IC50 = 5300000.0 nM -
CHEMBL440702 IC50 = 2700000.0 nM -