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Assay Detail

CHEMBL4388228

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

Binding
Inhibition of Leishmania major pteridine reductase 1 using di-hydrobiopterine as substrate in presence of NADPH
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Leishmania major
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Pteridine reductase 1 (CHEMBL6194)
Type SINGLE PROTEIN
Organism Leishmania major

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 32 4.57 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95463 1 5.72
CHEMBL4552119 1 5.61
CHEMBL4582026 1 5.46
CHEMBL4439011 1 5.00
CHEMBL4564287 1 4.91
CHEMBL36 PYRIMETHAMINE 4.0 1 4.87
CHEMBL4458858 1 4.82
CHEMBL4441552 1 4.82
CHEMBL4583705 1 4.82
CHEMBL4581650 1 4.72
CHEMBL4562350 1 4.52
CHEMBL4456198 1 4.52
CHEMBL4566383 1 4.50
CHEMBL432942 1 4.48
CHEMBL4579215 1 4.44
CHEMBL4453795 1 4.43
CHEMBL4577695 1 4.32
CHEMBL4476655 1 4.30
CHEMBL4469761 1 4.21
CHEMBL4460492 1 4.19
CHEMBL4540341 1 4.18
CHEMBL4446494 1 4.18
CHEMBL4561783 1 4.13
CHEMBL4475811 1 4.09
CHEMBL4468228 1 4.06
CHEMBL4435791 1 4.05
CHEMBL744 RILUZOLE 4.0 1 4.03
CHEMBL4465714 1 -
CHEMBL2386433 1 -
CHEMBL4528355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95463 IC50 = 1900.0 nM 5.72
CHEMBL4552119 IC50 = 2480.0 nM 5.61
CHEMBL4582026 IC50 = 3510.0 nM 5.46
CHEMBL4439011 IC50 = 10000.0 nM 5.00
CHEMBL4564287 IC50 = 12400.0 nM 4.91
CHEMBL36 PYRIMETHAMINE IC50 = 13600.0 nM 4.87
CHEMBL4458858 IC50 = 15300.0 nM 4.82
CHEMBL4441552 IC50 = 15100.0 nM 4.82
CHEMBL4583705 IC50 = 15200.0 nM 4.82
CHEMBL4581650 IC50 = 18900.0 nM 4.72
CHEMBL4562350 IC50 = 30000.0 nM 4.52
CHEMBL4456198 IC50 = 30100.0 nM 4.52
CHEMBL4566383 IC50 = 31900.0 nM 4.50
CHEMBL432942 IC50 = 32900.0 nM 4.48
CHEMBL4579215 IC50 = 36000.0 nM 4.44
CHEMBL4453795 IC50 = 36800.0 nM 4.43
CHEMBL4577695 IC50 = 47600.0 nM 4.32
CHEMBL4476655 IC50 = 50000.0 nM 4.30
CHEMBL4469761 IC50 = 61300.0 nM 4.21
CHEMBL4460492 IC50 = 64700.0 nM 4.19
CHEMBL4540341 IC50 = 66600.0 nM 4.18
CHEMBL4446494 IC50 = 65900.0 nM 4.18
CHEMBL4561783 IC50 = 73300.0 nM 4.13
CHEMBL4475811 IC50 = 81000.0 nM 4.09
CHEMBL4468228 IC50 = 86500.0 nM 4.06
CHEMBL4435791 IC50 = 88500.0 nM 4.05
CHEMBL744 RILUZOLE IC50 = 94100.0 nM 4.03
CHEMBL4465714 IC50 - -
CHEMBL2386433 IC50 - -
CHEMBL4528355 IC50 - -
CHEMBL4462566 IC50 - -
CHEMBL4444333 IC50 - -