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Compound Detail

CHEMBL475346

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Clc1ccc(Nc2nc3ccccc3c3nc(C4CCCCC4)[nH]c23)cc1Cl

Basic Information

ChEMBL ID CHEMBL475346
Phase Preclinical
Structure Type MOL
InChI Key UWJVRSIGHHSDSJ-UHFFFAOYSA-N

Known Names

LUF-6000
1
Targets
4
Activities
2
Assay Types
0
PK Parameters
15
Publications
1
Known Names

Molecular Properties

411.3
MW (Da)
7.21
ALogP
3
HBA
2
HBD
53.6
PSA (Ų)
0.37
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20Cl2N4
MW 411.34
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.16

Activity Summary

EC50 3 meas. best 7.46
Ki 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A3
CHEMBL256
EC50 7.46 7.3133 34.7 3
Adenosine receptor A3
CHEMBL256
Ki 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38959401 10.1021/acs.jmedchem.4c00944 Adenosine receptor A3 10
36367749 10.1021/acs.jmedchem.2c01170 Adenosine receptor A3 4
16722654 10.1021/jm060086s Adenosine receptor A3 3
19284749 10.1021/jm801659w Adenosine receptor A3 3
19161279 10.1021/jm8014052 Adenosine receptor A3 3
19161279 10.1021/jm8014052 Adenosine receptor A1 2
16722654 10.1021/jm060086s Adenosine receptor A1 1
16722654 10.1021/jm060086s Adenosine receptor A2a 1
16722654 10.1021/jm060086s Adenosine receptor A2b 1
19284749 10.1021/jm801659w Adenosine receptor A1 1
19284749 10.1021/jm801659w Adenosine receptor A2a 1
19161279 10.1021/jm8014052 Adenosine receptor A2a 1
19161279 10.1021/jm8014052 Adenosine receptor A2b 1
22468757 10.1021/jm300087j Adenosine receptor A3 1
25868747 10.1016/j.bmc.2015.03.039 Adenosine receptor A3 1

Data from ChEMBL 36 via Core Engine