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Compound Detail

CHEMBL591434

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CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)([O-])OP(=O)([O-])CP(=O)([O-])OP(=O)([O-])OC[C@H]4O[C@@H](n5cnc6c(N)nc(SC)nc65)[C@H](O)[C@@H]4O)[C@@H](O)[C@H]3O)c2n1.[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL591434
Phase Preclinical
Structure Type MOL
InChI Key ZCTGJDSLYNLUNE-QBVJLQLXSA-J
Parent Compound CHEMBL1615708
Active Moiety CHEMBL1615708
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

926.6
MW (Da)
-0.89
ALogP
26
HBA
10
HBD
424.7
PSA (Ų)
0.04
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30N10Na4O18P4S2
MW 1014.54
Aromatic Rings 4
Heavy Atoms 57
NP-Likeness 0.35

Activity Summary

EC50 1 meas. best 6.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 1
CHEMBL4315
EC50 6.34 6.34 460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 1 EC50 = 460.0 nM 6.34 Agonist activity at G-protein coupled P2Y1 receptor expressed in human 1321N1 ce... 20175517

Literature References

PubMed DOI Target Context # Activities
20175517 10.1021/jm901621h P2Y purinoceptor 1 1
20175517 10.1021/jm901621h ADMET 1

Data from ChEMBL 36 via Core Engine