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Compound Detail

CHEMBL610859

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O=C(Cc1ccc(NC(=O)Cc2ccc(Nc3ncnc4c3ncn4C3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1)NCC/N=C(/S)Nc1ccc2c(c1)C(=O)CC21c2ccc(O)cc2Oc2cc(O)ccc21

Basic Information

ChEMBL ID CHEMBL610859
Phase Preclinical
Structure Type MOL
InChI Key GQZABZLRWAKBEM-VQNJEBINSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

964.0
MW (Da)
4.86
ALogP
16
HBA
10
HBD
274.9
PSA (Ų)
0.03
QED
3
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C50H45N9O10S
MW 964.03
Aromatic Rings 7
Heavy Atoms 70
NP-Likeness 0.03

Activity Summary

Ki 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A1
CHEMBL318
Ki 8.15 8.15 7.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A1 Ki = 7.1 nM 8.15 Binding affinity for Adenosine A1 receptor using [3H]- CHA or [3H]- PIA 1738138

Literature References

PubMed DOI Target Context # Activities
1738138 10.1021/jm00081a001 Adenosine receptor A1 1

Data from ChEMBL 36 via Core Engine