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Compound Detail

CHEMBL6877

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Nc1nc(N)c2cc(Sc3ccc(Cl)c(Cl)c3)ccc2n1

Basic Information

ChEMBL ID CHEMBL6877
Phase Preclinical
Structure Type MOL
InChI Key QNNPAYVFMMNZIX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

337.2
MW (Da)
4.25
ALogP
5
HBA
2
HBD
77.8
PSA (Ų)
0.73
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H10Cl2N4S
MW 337.24
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.19

Activity Summary

IC50 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2363
IC50 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dihydrofolate reductase IC50 = 10.96 nM 7.96 Inhibitory activity against dihydrofolate reductase of rat liver 7277385

Literature References

PubMed DOI Target Context # Activities
102792 10.1021/jm00208a010 Plasmodium berghei 14
117107 10.1021/jm00196a019 Plasmodium gallinaceum 8
102792 10.1021/jm00208a010 Plasmodium gallinaceum 2
6737433 10.1021/jm00373a016 Dihydrofolate reductase 1
6864738 10.1021/jm00361a012 Dihydrofolate reductase 1
7392027 10.1021/jm00180a004 Dihydrofolate reductase 1
7120278 10.1021/jm00350a003 Dihydrofolate reductase 1
7277385 10.1021/jm00139a009 Dihydrofolate reductase 1
1271401 10.1021/jm00227a006 Dihydrofolate reductase 1
319234 10.1021/jm00211a020 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine