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Compound Detail

CHEMBL4078610

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O=c1[nH]c(=S)c(C2c3ccccc3C=Cc3ccccc32)cn1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4078610
Phase Preclinical
Structure Type MOL
InChI Key FXCUYHQWYSLSAA-KTDPBYDISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

450.5
MW (Da)
2.18
ALogP
7
HBA
4
HBD
107.7
PSA (Ų)
0.36
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N2O5S
MW 450.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.70

Activity Summary

Kd 1 meas. best 4.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 2
CHEMBL4398
Kd 4.7 4.7 19952.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 2 Kd = 19952.62 nM 4.7 Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as i... 28958619

Literature References

PubMed DOI Target Context # Activities
28958619 10.1016/j.bmcl.2017.09.043 P2Y purinoceptor 2 1

Data from ChEMBL 36 via Core Engine