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Compound Detail

CHEMBL601711

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[BH3-]P(=O)(OC[C@H]1O[C@@H](n2cnc3c(N)nc(SC)nc32)[C@H](O)[C@@H]1O)OP(=O)([O-])OP(=O)([O-])[O-].[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL601711
Phase Preclinical
Structure Type MOL
InChI Key WBNGHUVHRVWRPJ-AGVJRWMFSA-K
Parent Compound CHEMBL2364572
Active Moiety CHEMBL2364572
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

549.1
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H17BN5Na4O12P3S
MW 639.04

Activity Summary

EC50 1 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 1
CHEMBL2497
EC50 8.59 8.59 2.6 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.9 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 1 EC50 = 2.6 nM 8.59 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 ADMET 2
12431066 10.1021/jm020251d P2Y purinoceptor 1 1

Data from ChEMBL 36 via Core Engine