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Compound Detail

CHEMBL4061457

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Cc1ncccc1OCc1cccc2nc(N)nc(N)c12

Basic Information

ChEMBL ID CHEMBL4061457
Phase Preclinical
Structure Type MOL
InChI Key DQAAUHWZLOHBJA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

281.3
MW (Da)
2.08
ALogP
6
HBA
2
HBD
99.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N5O
MW 281.32
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.82

Activity Summary

IC50 1 meas. best 9.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
m7GpppX diphosphatase
CHEMBL1949488
IC50 9.57 9.57 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
m7GpppX diphosphatase IC50 = 0.27 nM 9.57 Inhibition of human DcpS assessed as increase in SMN2 promoter activity 28257199

Literature References

PubMed DOI Target Context # Activities
28257199 10.1021/acs.jmedchem.7b00124 ADMET 3
28257199 10.1021/acs.jmedchem.7b00124 Unchecked 3
28257199 10.1021/acs.jmedchem.7b00124 Liver 2
28257199 10.1021/acs.jmedchem.7b00124 No relevant target 2
28257199 10.1021/acs.jmedchem.7b00124 m7GpppX diphosphatase 1
28257199 10.1021/acs.jmedchem.7b00124 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine