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Assay Detail

CHEMBL4388239

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

ADMET
Inhibition of human CYP2C9 expressed in baculovirus infected insect cells using beetle D-luciferin as substrate preincubated for 30 mins followed by NADPH addition and measured after 30 mins by CYP450-Glo assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
Linciano P, Pozzi C, Iacono LD, di Pisa F, Landi G, Bonucci A, Gul S, Kuzikov M, Ellinger B, Witt G, Santarem N, Baptista C, Franco C, Moraes CB, Müller W, Wittig U, Luciani R, Sesenna A, Quotadamo A, Ferrari S, Pöhner I, Cordeiro-da-Silva A, Mangani S, Costantino L, Costi MP.
J Med Chem (2019) 62 : 3989 -4012
PubMed 30908048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446494 1 5.00
CHEMBL4581650 1 5.00
CHEMBL4545398 1 5.00
CHEMBL4564287 1 5.00
CHEMBL4579215 1 5.00
CHEMBL4549839 1 -
CHEMBL4566383 1 -
CHEMBL4583705 1 -
CHEMBL4453795 1 -
CHEMBL4456198 1 -
CHEMBL55 PENTAMIDINE 4.0 1 -
CHEMBL4439011 1 -
CHEMBL744 RILUZOLE 4.0 1 -
CHEMBL2386433 1 -
CHEMBL4465714 1 -
CHEMBL4468228 1 -
CHEMBL4540341 1 -
CHEMBL4552119 1 -
CHEMBL4462566 1 -
CHEMBL4452773 1 -
CHEMBL4444333 1 -
CHEMBL4528355 1 -
CHEMBL4554707 1 -
CHEMBL4435791 1 -
CHEMBL4460492 1 -
CHEMBL4582026 1 -
CHEMBL4554726 1 -
CHEMBL4452155 1 -
CHEMBL4469761 1 -
CHEMBL4561783 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446494 IC50 = 10000.0 nM 5.00
CHEMBL4581650 IC50 = 10000.0 nM 5.00
CHEMBL4545398 IC50 = 10000.0 nM 5.00
CHEMBL4564287 IC50 = 10000.0 nM 5.00
CHEMBL4579215 IC50 = 10000.0 nM 5.00
CHEMBL744 RILUZOLE IC50 > 25000.0 nM -
CHEMBL97797 IC50 > 25000.0 nM -
CHEMBL2386433 IC50 > 25000.0 nM -
CHEMBL4465714 IC50 > 25000.0 nM -
CHEMBL4468228 IC50 > 25000.0 nM -
CHEMBL4540341 IC50 > 25000.0 nM -
CHEMBL4566383 IC50 < 10000.0 nM -
CHEMBL4592124 IC50 > 25000.0 nM -
CHEMBL95463 IC50 > 25000.0 nM -
CHEMBL4475811 IC50 > 25000.0 nM -
CHEMBL4458858 IC50 > 25000.0 nM -
CHEMBL4577695 IC50 < 10000.0 nM -
CHEMBL4441552 IC50 > 25000.0 nM -
CHEMBL4562350 IC50 < 10000.0 nM -
CHEMBL432942 IC50 > 25000.0 nM -
CHEMBL4440584 IC50 > 25000.0 nM -
CHEMBL4581441 IC50 > 25000.0 nM -
CHEMBL4464690 IC50 > 25000.0 nM -
CHEMBL4476655 IC50 < 10000.0 nM -
CHEMBL4444333 IC50 < 10000.0 nM -
CHEMBL4561783 IC50 > 25000.0 nM -
CHEMBL4469761 IC50 > 25000.0 nM -
CHEMBL4452155 IC50 > 25000.0 nM -
CHEMBL4554726 IC50 > 25000.0 nM -
CHEMBL4582026 IC50 > 25000.0 nM -
CHEMBL4460492 IC50 > 25000.0 nM -
CHEMBL4435791 IC50 < 10000.0 nM -
CHEMBL4554707 IC50 > 25000.0 nM -
CHEMBL4528355 IC50 > 25000.0 nM -
CHEMBL4439011 IC50 > 25000.0 nM -
CHEMBL4452773 IC50 > 25000.0 nM -
CHEMBL4462566 IC50 < 10000.0 nM -
CHEMBL4552119 IC50 > 25000.0 nM -
CHEMBL4549839 IC50 > 25000.0 nM -
CHEMBL4583705 IC50 < 10000.0 nM -
CHEMBL4453795 IC50 > 25000.0 nM -
CHEMBL4456198 IC50 > 25000.0 nM -
CHEMBL55 PENTAMIDINE IC50 > 25000.0 nM -