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Compound Detail

CHEMBL4128532

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O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCNc1nc2c(s1)C=Cc1cc(Cl)ccc1C2c1cn(Cc2nc(C(=O)Nc3nnn[nH]3)cs2)c(=O)[nH]c1=S

Basic Information

ChEMBL ID CHEMBL4128532
Phase Preclinical
Structure Type MOL
InChI Key VRVJYJYBTMSOOF-KPKJPENVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

1242.7
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C56H51BClF2N15O6S4
MW 1242.65

Activity Summary

Kd 1 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 2
CHEMBL4398
Kd 6.89 6.89 128.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 2 Kd = 128.82 nM 6.89 Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in ... 29558126

Literature References

PubMed DOI Target Context # Activities
29558126 10.1021/acs.jmedchem.8b00139 P2Y purinoceptor 2 4
29558126 10.1021/acs.jmedchem.8b00139 Unchecked 1

Data from ChEMBL 36 via Core Engine