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Compound Detail

CHEMBL3612932

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CCCNc1nc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12

Basic Information

ChEMBL ID CHEMBL3612932
Phase Preclinical
Structure Type MOL
InChI Key CPDWVNNYXONUCC-YWNJHDJRSA-N
6
Targets
8
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

487.0
MW (Da)
1.79
ALogP
9
HBA
4
HBD
125.2
PSA (Ų)
0.41
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23ClN6O3S
MW 486.99
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.13

Activity Summary

Ki 6 meas. best 8.96
EC50 2 meas. best 6.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A3
CHEMBL256
Ki 8.96 8.96 1.1 2
Adenosine receptor A3
CHEMBL3611963
Ki 8.24 8.24 5.8 1
Adenosine receptor A3
CHEMBL1075269
Ki 8.17 8.17 6.8 2
Sodium-dependent noradrenaline transporter
CHEMBL222
EC50 6.05 6.05 900.0 1
Sodium-dependent dopamine transporter
CHEMBL238
EC50 5.95 5.95 1120.0 1
Beta-3 adrenergic receptor
CHEMBL246
Ki 5.84 5.84 1440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28319392 10.1021/acs.jmedchem.7b00141 Sodium-dependent dopamine transporter 6
26191370 10.1021/acsmedchemlett.5b00150 Mus musculus 4
28319392 10.1021/acs.jmedchem.7b00141 Sodium-dependent noradrenaline transporter 4
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A3 3
28319392 10.1021/acs.jmedchem.7b00141 Sodium-dependent serotonin transporter 3
30568760 10.1039/C8MD00317C Adenosine receptor A3 2
26191370 10.1021/acsmedchemlett.5b00150 5-hydroxytryptamine receptor 2B 1
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A2b 1
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A2a 1
26191370 10.1021/acsmedchemlett.5b00150 Adenosine receptor A1 1
28319392 10.1021/acs.jmedchem.7b00141 Beta-3 adrenergic receptor 1
30568760 10.1039/C8MD00317C Adenosine receptor A2a 1
30568760 10.1039/C8MD00317C Adenosine receptor A1 1
33062176 10.1021/acsmedchemlett.9b00637 Beta-3 adrenergic receptor 1
34825182 10.1039/D1MD00167A Adenosine receptor A1 1

Data from ChEMBL 36 via Core Engine