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Compound Detail

CHEMBL191071

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COc1cc(Cc2cnc(N)nc2N)cc(C#CCCC(=O)O)c1Br

Basic Information

ChEMBL ID CHEMBL191071
Phase Preclinical
Structure Type MOL
InChI Key DWQGRIVGUVJVRF-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

405.2
MW (Da)
2.22
ALogP
6
HBA
3
HBD
124.3
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17BrN4O3
MW 405.25
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 0.08

Activity Summary

IC50 4 meas. best 9.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL5457
IC50 9.33 9.33 0.5 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 7.82 7.82 15.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 7.15 7.15 71.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 6.2 6.2 630.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15974594 10.1021/jm0581718 Dihydrofolate reductase 3
15974594 10.1021/jm0581718 Bifunctional dihydrofolate reductase-thymidylate synthase 1
15974594 10.1021/jm0581718 Dihydrofolate reductase; P. carinii vs rat 1
15974594 10.1021/jm0581718 Dihydrofolate reductase; T. gondii vs rat 1
15974594 10.1021/jm0581718 Unchecked 1

Data from ChEMBL 36 via Core Engine