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Assay Detail

CHEMBL2185822

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

Binding
Inhibition of Leishmania major PTR1 by spectrophotometric assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Leishmania
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors.
Corona P, Gibellini F, Cavalli A, Saxena P, Carta A, Loriga M, Luciani R, Paglietti G, Guerrieri D, Nerini E, Gupta S, Hannaert V, Michels PA, Ferrari S, Costi PM.
J Med Chem (2012) 55 : 8318 -8329
PubMed 22946585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.85 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178602 1 7.52
CHEMBL1232702 1 7.43
CHEMBL2178603 1 7.22
CHEMBL2177120 1 7.11
CHEMBL2178601 1 7.00
CHEMBL1232399 1 7.00
CHEMBL34259 METHOTREXATE 4.0 1 6.75
CHEMBL2178600 1 6.68
CHEMBL2178599 1 6.41
CHEMBL2178604 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178602 Ki = 30.0 nM 7.52
CHEMBL1232702 Ki = 37.0 nM 7.43
CHEMBL2178603 Ki = 60.0 nM 7.22
CHEMBL2177120 Ki = 78.0 nM 7.11
CHEMBL2178601 Ki = 100.0 nM 7.00
CHEMBL1232399 Ki = 100.0 nM 7.00
CHEMBL34259 METHOTREXATE Ki = 180.0 nM 6.75
CHEMBL2178600 Ki = 210.0 nM 6.68
CHEMBL2178599 Ki = 390.0 nM 6.41
CHEMBL2178604 Ki = 4170.0 nM 5.38