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Compound Detail

CHEMBL5562824

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CCOc1ccc([C@@H](C)Nc2nc(N3CCN(C(C)=O)CC3)nc3c2CN(C(C)C)C3=O)cc1Cl

Basic Information

ChEMBL ID CHEMBL5562824
Phase Preclinical
Structure Type MOL
InChI Key MKFFNEABSLQYPM-MRXNPFEDSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

501.0
MW (Da)
3.73
ALogP
7
HBA
1
HBD
90.9
PSA (Ų)
0.62
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33ClN6O3
MW 501.03
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.45

Activity Summary

IC50 2 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 7.43 7.43 37.0 1
P2X2/P2X3 receptor
CHEMBL3137277
IC50 6.26 6.26 547.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 37.0 nM 7.43 Antagonist activity at human P2X3 receptor 39102524
P2X2/P2X3 receptor IC50 = 547.2 nM 6.26 Antagonist activity at rat P2X2/3 receptor 39102524

Literature References

PubMed DOI Target Context # Activities
39102524 10.1021/acs.jmedchem.4c01214 P2X purinoceptor 3 1
39102524 10.1021/acs.jmedchem.4c01214 P2X2/P2X3 receptor 1

Data from ChEMBL 36 via Core Engine