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Compound Detail

CHEMBL33922

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COc1ccc(C#CCCCCC(=O)O)cc1Cc1cnc(N)nc1N

Basic Information

ChEMBL ID CHEMBL33922
Phase Preclinical
Structure Type MOL
InChI Key CIUYZEMTWPMSNU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

354.4
MW (Da)
2.24
ALogP
6
HBA
3
HBD
124.3
PSA (Ų)
0.51
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22N4O3
MW 354.41
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.12

Activity Summary

IC50 4 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL5457
IC50 7.39 7.39 41.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 7.14 7.14 72.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 6.06 6.06 870.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14998335 10.1021/jm030438k Mycobacterium avium 8
12699390 10.1021/jm020466n Dihydrofolate reductase 3
12699390 10.1021/jm020466n Bifunctional dihydrofolate reductase-thymidylate synthase 1
12699390 10.1021/jm020466n Dihydrofolate reductase; P. carinii vs rat 1
12699390 10.1021/jm020466n Dihydrofolate reductase; T. gondii vs rat 1
12699390 10.1021/jm020466n Unchecked 1

Data from ChEMBL 36 via Core Engine