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Compound Detail

CHEMBL3612939

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CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)cc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O

Basic Information

ChEMBL ID CHEMBL3612939
Phase Preclinical
Structure Type MOL
InChI Key DVEWTVCBLKZYMV-NEWQXWLQSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

457.9
MW (Da)
1.62
ALogP
8
HBA
4
HBD
112.3
PSA (Ų)
0.44
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 C21H20ClN5O3S
MW 457.94
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.01

Activity Summary

Ki 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A3
CHEMBL256
Ki 8.52 8.52 3.0 1
Adenosine receptor A3
CHEMBL1075269
Ki 7.51 7.51 31.0 1
Adenosine receptor A3
CHEMBL3611963
Ki 7.12 7.12 75.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26191370 10.1021/acsmedchemlett.5b00150 Mus musculus 4
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A3 3
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A2a 1
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A1 1
33062176 10.1021/acsmedchemlett.9b00637 Beta-3 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine