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Compound Detail

CHEMBL2011116

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COc1cc(OC(F)(F)F)ccc1CNc1nc(N2CCN(C(C)=O)CC2)nc2c1CN(C(C)C)C2=O

Basic Information

ChEMBL ID CHEMBL2011116
Phase Preclinical
Structure Type MOL
InChI Key BGLNPGCRIGALDL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

522.5
MW (Da)
3.03
ALogP
8
HBA
1
HBD
100.1
PSA (Ų)
0.59
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29F3N6O4
MW 522.53
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 7.17 7.17 67.0 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 = 67.0 nM 7.17 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