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Compound Detail

CHEMBL2364736

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CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])[O-])[C@@H](O)[C@H]3O)c2n1.[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL2364736
Phase Preclinical
Structure Type MOL
InChI Key UEEFBRHXFDJPTA-KWIZKVQNSA-J
Parent Compound CHEMBL336208
Active Moiety CHEMBL336208
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

553.3
MW (Da)
-0.91
ALogP
15
HBA
7
HBD
279.1
PSA (Ų)
0.11
QED
3
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H14N5Na4O13P3S
MW 641.20
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.84

Activity Summary

EC50 1 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 1
CHEMBL2497
EC50 8.35 8.35 4.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 1 EC50 = 4.5 nM 8.35 Agonists activity was evaluated by release of [Ca2+] release of HEK 293 cells st... 12431066

Literature References

PubMed DOI Target Context # Activities
12431066 10.1021/jm020251d Bos taurus 2
12431066 10.1021/jm020251d P2Y purinoceptor 1 1

Data from ChEMBL 36 via Core Engine