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Compound Detail

CHEMBL500634

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[3H]C([3H])(CN1CCN(C(=O)c2cc3c(NCCNC(C)=O)nc(-c4ccccc4)nc3[nH]2)CC1)C([3H])([3H])c1ccccc1

Basic Information

ChEMBL ID CHEMBL500634
Phase Preclinical
Structure Type MOL
InChI Key MIUCZFWBCFZKEU-INIJAGOKSA-N
Parent Compound CHEMBL485862
Active Moiety CHEMBL485862
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

525.7
MW (Da)
3.56
ALogP
6
HBA
3
HBD
106.2
PSA (Ų)
0.27
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35N7O2
MW 533.69
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.33

Activity Summary

Kd 1 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2b
CHEMBL255
Kd 9.77 9.77 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine receptor A2b Kd = 0.17 nM 9.77 Binding affinity to human adenosine A2B receptor 19569717

Literature References

PubMed DOI Target Context # Activities
19569717 10.1021/jm900413e Adenosine receptor A2b 1

Data from ChEMBL 36 via Core Engine