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Compound Detail

CHEMBL354055

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CCCN(Cc1cnc2nc(N)nc(N)c2n1)c1ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL354055
Phase Preclinical
Structure Type MOL
InChI Key OXKVXUQXNRYHMZ-UHFFFAOYSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

482.5
MW (Da)
1.05
ALogP
10
HBA
5
HBD
210.5
PSA (Ų)
0.26
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N8O5
MW 482.50
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.59

Activity Summary

Ki 2 meas.
IC50 1 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 8.66 8.66 2.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
L1210 IC50 = 2.2 nM 8.66 In vitro inhibition of L1210 cell growth in rodent neoplastic cells 7108907

Literature References

PubMed DOI Target Context # Activities
7108907 10.1021/jm00349a024 Mus musculus 8
7108907 10.1021/jm00349a024 L1210 6
7108907 10.1021/jm00349a024 Dihydrofolate reductase 1
7108907 10.1021/jm00349a024 Unchecked 1
7108907 10.1021/jm00349a024 Ehrlich 1
11465411 10.1023/a:1011064806507 ATP-binding cassette sub-family C member 2 1

Data from ChEMBL 36 via Core Engine