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Compound Detail

CHEMBL3707395

ELAFIBRANOR
💊 Approved Drug
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💊 Approved Drug
CSc1ccc(C(=O)/C=C/c2cc(C)c(OC(C)(C)C(=O)O)c(C)c2)cc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3707395
Name ELAFIBRANOR
Phase Approved
Structure Type MOL
InChI Key AFLFKFHDSCQHOL-IZZDOVSWSA-N
Therapeutic ✓ Yes

Known Names

Elafibranor GFT-505 Gft505 Iqirvo
4
Targets
20
Activities
2
Assay Types
2
PK Parameters
20
Publications
4
Known Names
7
Indications
2
Mechanisms

Molecular Properties

384.5
MW (Da)
5.16
ALogP
4
HBA
1
HBD
63.6
PSA (Ų)
0.41
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2024
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Natural Product First in Class
USAN Year 2015

Extended Properties

Molecular Formula C22H24O4S
MW 384.50
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.21

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Peroxisome proliferator-activated receptor alpha agonist AGONIST Peroxisome proliferator-activated receptor alpha ✓ ✓
Peroxisome proliferator-activated receptor delta agonist AGONIST Peroxisome proliferator-activated receptor delta ✓ ✓

Indications

Cholangitis Liver Cirrhosis, Biliary Cholangitis, Sclerosing Diabetes Mellitus, Type 2 Non-alcoholic Fatty Liver Disease Non-alcoholic Fatty Liver Disease Liver Diseases

ATC Classification

A05AX06
elafibranor
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: BILE AND LIVER THERAPY

Activity Summary

EC50 19 meas. best 8.0
IC50 1 meas. best 4.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor alpha
CHEMBL239
 EC50 8.0 6.79 10.0 7
Peroxisome proliferator-activated receptor delta
CHEMBL3979
 EC50 8.0 6.7383 10.0 6
Peroxisome proliferator-activated receptor gamma
CHEMBL235
 EC50 6.76 5.9167 175.0 6
NACHT, LRR and PYD domains-containing protein 3
CHEMBL3779755
 IC50 4.4 4.4 39600.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 116.35 mL.min-1.kg-1 Homo sapiens
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Peroxisome proliferator-activated receptor delta EC50 = 10.0 nM 8.0 Agonist activity at PPARdelta (unknown origin) 31930920
Peroxisome proliferator-activated receptor alpha EC50 = 10.0 nM 8.0 Agonist activity at PPARalpha (unknown origin) 31930920
Peroxisome proliferator-activated receptor alpha EC50 = 45.0 nM 7.35 Agonist activity at PPARalpha (unknown origin) assessed as transcriptional activ... 32339855
Peroxisome proliferator-activated receptor delta EC50 = 115.0 nM 6.94 Agonist activity at PPARbeta (unknown origin) incubated for 3 to 16 hrs by pathh... 31312410
Peroxisome proliferator-activated receptor alpha EC50 = 130.0 nM 6.89 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Peroxisome proliferator-activated receptor gamma EC50 = 175.0 nM 6.76 Agonist activity at PPARgamma (unknown origin) assessed as transcriptional activ... 32339855
Peroxisome proliferator-activated receptor delta EC50 = 210.0 nM 6.68 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Peroxisome proliferator-activated receptor alpha EC50 = 225.0 nM 6.65 Agonist activity at PPARalpha (unknown origin) incubated for 3 to 16 hrs by path... 31312410
Peroxisome proliferator-activated receptor delta EC50 = 249.0 nM 6.6 Agonist activity at human PPARdelta transfected in human HEK293 cells incubated ... 34455359
Peroxisome proliferator-activated receptor alpha EC50 = 375.0 nM 6.43 Agonist activity at human PPARalpha transfected in human HepG2 cells incubated f... 34455359
Peroxisome proliferator-activated receptor gamma EC50 = 410.0 nM 6.39 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Peroxisome proliferator-activated receptor delta EC50 = 730.0 nM 6.14 Agonist activity at human Gal4 fused PPARdelta LBD expressed in COS-7 cells incu... 33784603
Peroxisome proliferator-activated receptor alpha EC50 = 760.0 nM 6.12 Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incu... 33784603
Peroxisome proliferator-activated receptor alpha EC50 = 820.3 nM 6.09 Agonist activity at PPARalpha (unknown origin) 35060744
Peroxisome proliferator-activated receptor delta EC50 = 842.9 nM 6.07 Agonist activity at PPARdelta (unknown origin) 35060744
Peroxisome proliferator-activated receptor gamma EC50 = 1843.8 nM 5.73 Agonist activity at PPARgamma (unknown origin) 35060744
Peroxisome proliferator-activated receptor gamma EC50 = 2116.0 nM 5.67 Agonist activity at PPARgamma (unknown origin) incubated for 3 to 16 hrs by path... 31312410
Peroxisome proliferator-activated receptor gamma EC50 = 2790.0 nM 5.55 Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incu... 33784603
Peroxisome proliferator-activated receptor gamma EC50 = 3962.0 nM 5.4 Agonist activity at human PPARgamma transfected in human HEK293 cells incubated ... 34455359
NACHT, LRR and PYD domains-containing protein 3 IC50 = 39600.0 nM 4.4 Inhibition of NLRP3 in mouse J774A.1 cells infected with FLA-ST assessed as inhi... 33845232

Literature References

PubMed DOI Target Context # Activities
37269672 10.1016/j.ejmech.2023.115510 Mus musculus 14
- 10.6019/CHEMBL5303304 U2OS 10
- 10.6019/CHEMBL5303304 Fibroblast 7
- 10.6019/CHEMBL5303304 HEK-293T 5
37269672 10.1016/j.ejmech.2023.115510 HepG2 4
- 10.6019/CHEMBL5724696 TERT-RPE1 4
31312410 10.1021/acsmedchemlett.9b00189 Rattus norvegicus 3
34455359 10.1016/j.ejmech.2021.113807 Peroxisome proliferator-activated receptor gamma 2
34455359 10.1016/j.ejmech.2021.113807 Peroxisome proliferator-activated receptor alpha 2
34455359 10.1016/j.ejmech.2021.113807 Peroxisome proliferator-activated receptor delta 2
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor alpha 2
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor delta 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor gamma 2
31312410 10.1021/acsmedchemlett.9b00189 Peroxisome proliferator-activated receptor alpha 2
31312410 10.1021/acsmedchemlett.9b00189 Peroxisome proliferator-activated receptor delta 2
31312410 10.1021/acsmedchemlett.9b00189 Peroxisome proliferator-activated receptor gamma 2
35060744 10.1021/acs.jmedchem.1c02002 ADMET 2

Data from ChEMBL 36 via Core Engine