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Compound Detail

CHEMBL1650282

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Nc1nnc(-c2ccc3[nH]nnc3c2)s1

Basic Information

ChEMBL ID CHEMBL1650282
Phase Preclinical
Structure Type MOL
InChI Key QEDRDOHUKCLXOP-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

218.2
MW (Da)
1.06
ALogP
6
HBA
2
HBD
93.4
PSA (Ų)
0.64
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C8H6N6S
MW 218.25
Aromatic Rings 3
Heavy Atoms 15
NP-Likeness -2.15

Activity Summary

IC50 1 meas.
Ki 1 meas. best 4.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Pteridine reductase 1
CHEMBL6194
Ki 4.62 4.62 24000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Pteridine reductase 1 Ki = 24000.0 nM 4.62 Inhibition of Leishmania major PTR1 by Lineweaver-Burk analysis 21126022

Literature References

PubMed DOI Target Context # Activities
21126022 10.1021/jm1010572 Pteridine reductase 1 3
21126022 10.1021/jm1010572 No relevant target 2
21126022 10.1021/jm1010572 MRC5 2
21126022 10.1021/jm1010572 Leishmania major 2
21126022 10.1021/jm1010572 Leishmania mexicana 2
21126022 10.1021/jm1010572 Dihydrofolate reductase 1
21126022 10.1021/jm1010572 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine