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Compound Detail

CHEMBL5095224

ELIAPIXANT
🧪 Phase II
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🧪 Phase II
Cc1cnc(-c2cc(O[C@@H]3CCOC3)cc(C(=O)N[C@H](C)c3cnc(C(F)(F)F)nc3)c2)s1

Basic Information

ChEMBL ID CHEMBL5095224
Name ELIAPIXANT
Phase Phase II
Structure Type MOL
InChI Key GTQPEQGDLVSFJO-CXAGYDPISA-N

Known Names

BAY 1817080 BAY-1817080 BAY1817080 Eliapixant
3
Targets
13
Activities
1
Assay Types
0
PK Parameters
3
Publications
4
Known Names
7
Indications

Molecular Properties

478.5
MW (Da)
4.59
ALogP
7
HBA
1
HBD
86.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Year 2021

Extended Properties

Molecular Formula C22H21F3N4O3S
MW 478.50
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.15

Indications

Cough Endometriosis Urinary Bladder, Overactive Chronic Cough Diabetic Neuropathies Neuralgia Pain

Activity Summary

IC50 13 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 8.1 7.7829 8.0 7
P2X purinoceptor 2
CHEMBL2531
IC50 6.79 6.79 163.0 2
P2X2/P2X3 heterotrimeric receptor
CHEMBL3831281
IC50 6.79 6.3425 163.0 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reducti... 35849939
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Antagonist activity at human P2X3 receptor expressed in 1321N1 cells assessed as... 39102524
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X purinoceptor 3 IC50 = 8.0 nM 8.1 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X2/P2X3 heterotrimeric receptor IC50 = 163.0 nM 6.79 Antagonist activity at human P2X2/3 receptor expressed in 1321N1 cells assessed ... 39102524
P2X purinoceptor 2 IC50 = 163.0 nM 6.79 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X purinoceptor 2 IC50 = 163.0 nM 6.79 Intracellular Calcium Measurement to Assess Antagonist Activity at Human P2X3 an... -
P2X2/P2X3 heterotrimeric receptor IC50 = 163.0 nM 6.79 Intracellular Calcium Measurement to Assess Antagonist Activity : A fluorescent ... -
P2X2/P2X3 heterotrimeric receptor IC50 = 163.0 nM 6.79 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X purinoceptor 3 IC50 = 1320.0 nM 5.88 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -
P2X2/P2X3 heterotrimeric receptor IC50 = 10000.0 nM 5.0 Biological Assay: A fluorescent imaging plate reader (FILEX/FLIPR station; Molec... -

Literature References

PubMed DOI Target Context # Activities
35849939 10.1016/j.ejmech.2022.114556 P2X purinoceptor 3 1
39102524 10.1021/acs.jmedchem.4c01214 P2X purinoceptor 3 1
39102524 10.1021/acs.jmedchem.4c01214 P2X2/P2X3 heterotrimeric receptor 1

Data from ChEMBL 36 via Core Engine