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Compound Detail

CHEMBL1222883

GSK1482160
Phase I
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Phase I
CN1C(=O)CC[C@H]1C(=O)NCc1cccc(C(F)(F)F)c1Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1222883
Name GSK1482160
Phase Phase I
Structure Type MOL
InChI Key BJEMSIVBBUBXMZ-JTQLQIEISA-N

Known Names

Gsk-1482160 Gsk1482160 GSK1482160A
3
Targets
14
Activities
2
Assay Types
20
PK Parameters
20
Publications
3
Known Names
1
Indications
1
Mechanisms

Molecular Properties

334.7
MW (Da)
2.60
ALogP
2
HBA
1
HBD
49.4
PSA (Ų)
0.92
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Extended Properties

Molecular Formula C14H14ClF3N2O2
MW 334.73
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -1.02

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
P2X purinoceptor 7 negative allosteric modulator NEGATIVE ALLOSTERIC MODULATOR P2X purinoceptor 7 ✓ ✓

Indications

Pain

Activity Summary

IC50 10 meas. best 8.5
Ki 4 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL4805
 Ki 8.51 7.9733 3.1 3
P2X purinoceptor 7
CHEMBL4805
 IC50 8.5 7.6917 3.2 6
P2X purinoceptor 7
CHEMBL2496
 IC50 6.6 6.2733 251.2 3
P2X purinoceptor 7
CHEMBL2496
 Ki 6.29 6.29 510.0 1
P2X purinoceptor 7
CHEMBL5183
 IC50 5.64 5.64 2300.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1216910000.0 ng.hr.mL-1 Rattus norvegicus
CL 9.0 mL.min-1.kg-1 Rattus norvegicus
CL 0.5 mL.min-1.g-1 Homo sapiens
CL 9.0 mL.min-1.kg-1 Rattus norvegicus
CL 14.0 mL.min-1.kg-1 Canis lupus familiaris
CL 17.0 mL.min-1.kg-1 Macaca mulatta
CL 2.8 mL.min-1.g-1 Homo sapiens
CL 5.0 mL.min-1.kg-1 Homo sapiens
CL 16.67 mL.min-1.kg-1 Rattus norvegicus
Cmax 2450.0 nM Rattus norvegicus
F 65.0 % Rattus norvegicus
F 57.0 % Macaca mulatta
F 65.0 % Rattus norvegicus
F 69.0 % Canis lupus familiaris
T1/2 1.5 hr Rattus norvegicus
T1/2 0.7 hr Canis lupus familiaris
T1/2 0.9 hr Macaca mulatta
T1/2 1.5 hr Rattus norvegicus
T1/2 13.33 hr Homo sapiens
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 Ki = 3.1 nM 8.51 Competitive displacement of [11C]GSK1482160 from human recombinant P2X7 receptor... 31005444
P2X purinoceptor 7 IC50 = 3.162 nM 8.5 Inhibition of human P2X7 receptor by ethidium bromide release assay 20673717
P2X purinoceptor 7 IC50 = 3.162 nM 8.5 Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells... 20934331
P2X purinoceptor 7 Ki = 5.7 nM 8.24 Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell ... 33822617
P2X purinoceptor 7 IC50 = 8.9 nM 8.05 Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed i... 31005444
P2X purinoceptor 7 IC50 = 20.0 nM 7.7 Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as... 33822617
P2X purinoceptor 7 Ki = 68.0 nM 7.17 Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell memb... 31525963
P2X purinoceptor 7 IC50 = 119.3 nM 6.92 Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction i... 31525963
P2X purinoceptor 7 IC50 = 251.19 nM 6.6 Antagonist activity at rat recombinant P2X7 receptor 20934331
P2X purinoceptor 7 IC50 = 316.23 nM 6.5 Inhibition of rat P2X7 receptor by ethidium bromide release assay 20673717
P2X purinoceptor 7 IC50 = 332.4 nM 6.48 Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell memb... 31525963
P2X purinoceptor 7 Ki = 510.0 nM 6.29 Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell me... 33822617
P2X purinoceptor 7 IC50 = 1900.0 nM 5.72 Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as i... 33822617
P2X purinoceptor 7 IC50 = 2300.0 nM 5.64 Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as... 33822617

Literature References

PubMed DOI Target Context # Activities
20673717 10.1016/j.bmcl.2010.07.033 Rattus norvegicus 9
31525963 10.1021/acs.jmedchem.9b00584 P2X purinoceptor 7 7
33822617 10.1021/acs.jmedchem.0c02249 P2X purinoceptor 7 5
33822617 10.1021/acs.jmedchem.0c02249 ADMET 4
31525963 10.1021/acs.jmedchem.9b00584 ADMET 4
20934331 10.1016/j.bmcl.2010.09.101 Rattus norvegicus 4
20934331 10.1016/j.bmcl.2010.09.101 Rhesus monkey 4
20934331 10.1016/j.bmcl.2010.09.101 Canis familiaris 4
20673717 10.1016/j.bmcl.2010.07.033 Plasma 3
20673717 10.1016/j.bmcl.2010.07.033 No relevant target 2
31005444 10.1016/j.bmcl.2019.04.018 P2X purinoceptor 7 2
20934331 10.1016/j.bmcl.2010.09.101 P2X purinoceptor 7 2
20673717 10.1016/j.bmcl.2010.07.033 Brain 2
20673717 10.1016/j.bmcl.2010.07.033 P2X purinoceptor 7 2
20673717 10.1016/j.bmcl.2010.07.033 Liver microsomes 1
20673717 10.1016/j.bmcl.2010.07.033 Cytochrome P450 3A4 1
20673717 10.1016/j.bmcl.2010.07.033 Cytochrome P450 2D6 1
20673717 10.1016/j.bmcl.2010.07.033 Cytochrome P450 2C19 1
20673717 10.1016/j.bmcl.2010.07.033 Cytochrome P450 2C9 1
31525963 10.1021/acs.jmedchem.9b00584 No relevant target 1

Data from ChEMBL 36 via Core Engine