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Compound Detail

CHEMBL2011124

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CCOc1ncc([C@@H](C)Nc2nc(N3CCN(C(C)=O)CC3)nc3c2CN(C(C)C)C3=O)cc1F

Basic Information

ChEMBL ID CHEMBL2011124
Phase Preclinical
Structure Type MOL
InChI Key LBGUGHRCONFPLR-OAHLLOKOSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
2.62
ALogP
8
HBA
1
HBD
103.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H32FN7O3
MW 485.56
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.44

Activity Summary

IC50 1 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 6.28 6.28 521.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 521.0 nM 6.28 Antagonist activity at human P2X3 receptor expressed in RLE cells assessed as in... 22370269

Literature References

PubMed DOI Target Context # Activities
22370269 10.1016/j.bmcl.2012.01.124 P2X purinoceptor 3 1
22370269 10.1016/j.bmcl.2012.01.124 No relevant target 1
22370269 10.1016/j.bmcl.2012.01.124 Liver microsomes 1

Data from ChEMBL 36 via Core Engine