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Compound Detail

CHEMBL283062

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CN(Cc1cnc2nc(N)nc(N)c2n1)c1ccc(C(=O)NC(CCCCCCC(=O)O)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL283062
Phase Preclinical
Structure Type MOL
InChI Key HBCSTDBQBDYRGS-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

510.6
MW (Da)
1.83
ALogP
10
HBA
5
HBD
210.5
PSA (Ų)
0.21
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N8O5
MW 510.56
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.40

Activity Summary

IC50 5 meas. best 8.92
Ki 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 8.92 8.92 1.2 1
Dihydrofolate reductase
CHEMBL4564
IC50 7.64 7.64 23.0 1
CCRF-CEM
CHEMBL382
IC50 6.82 6.03 150.0 2
L1210 ( R81)
CHEMBL614710
IC50 4.17 4.17 68000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2898531 10.1021/jm00402a014 L1210 17
2898531 10.1021/jm00402a014 CCRF-CEM 2
2898531 10.1021/jm00402a014 Folylpolyglutamate synthase, mitochondrial 2
2898531 10.1021/jm00402a014 Dihydrofolate reductase 1
2898531 10.1021/jm00402a014 L1210 ( R81) 1

Data from ChEMBL 36 via Core Engine