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Compound Detail

CHEMBL1256935

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Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])[O-])[C@@H](O)[C@H]1O.[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL1256935
Phase Preclinical
Structure Type MOL
InChI Key JGKMWMQAWOVZHJ-ZVQJTLEUSA-J
Parent Compound CHEMBL1368696
Active Moiety CHEMBL1368696
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
-0.98
ALogP
14
HBA
7
HBD
279.1
PSA (Ų)
0.16
QED
3
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H11ClN5Na4O13P3
MW 629.56
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 1.16

Activity Summary

EC50 1 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 1
CHEMBL2497
EC50 8.44 8.44 3.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 1 EC50 = 3.6 nM 8.44 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
17417631 10.1038/nchembio873 Unchecked 1

Data from ChEMBL 36 via Core Engine