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Compound Detail

CHEMBL2011114

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CC(=O)N1CCN(c2nc(NCc3ccc(C(F)(F)F)cc3)c3c(n2)C(=O)N(C(C)C)C3)CC1

Basic Information

ChEMBL ID CHEMBL2011114
Phase Preclinical
Structure Type MOL
InChI Key APWGKCNSBHECJN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
3.14
ALogP
6
HBA
1
HBD
81.7
PSA (Ų)
0.71
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 C23H27F3N6O2
MW 476.50
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.37

Activity Summary

IC50 1 meas. best 5.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 5.9 5.9 1271.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 31.0 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 = 1271.0 nM 5.9 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