General
Preferred name
SAR443122
Synonyms
eclitasertib ()
DNL-758 ()
SAR-443122 ()
DNL758 ()
P&D ID
PD133903
CAS
2125450-76-0
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Drug indication
Cutaneous lupus erythematosus
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of 0.0375 ¦Ì¦¬[1].
PRICE 310
DESCRIPTION Eclitasertib is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1, IC50 of <1 ???).
DESCRIPTION This chemical structure for eclitasertib (as the IUPAC name) was obtained from the special release of proposed INNs for COVID-related therapeutics that was published by the WHO in October 2020. The INN structure was identified as being identical to example 42 from Denali Therapeutics' patent WO2017136727A2. Denali claim this compound as a kinase inhibitor, and the INN application refers to it as a RIP kinase inhibitor. Based on Denali's initiation of their RIPK1 inhibitor DNL758 (a.k.a. SAR443122) in clinical trial in COVID-19 patients, we speculated that example 42, DNL758/SAR443122 and eclitasertib were one and the same. As of August 2025, we have been able to align SAR443122 with eclitasertib, and tangentially link to the chemical structure via the WHO INN record for eclitasertib. (GtoPdb)
DESCRIPTION Eclitasertib is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1, IC50 of <1 µΜ). (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
6
ChEMBL Drugs
CHEMBL4861471
DrugBank
DB16492
Guide to Pharmacology
11308
MedChem Express Bioactive Compound Library
HY-114371
PKIDB
TargetMol Bioactive Compound Library
T9702
External IDs
14
Properties
(calculated by RDKit )
Molecular Weight
378.14
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
0.94
TPSA
113.1
Fraction CSP3
0.21
Chiral centers
1.0
Largest ring
7.0
QED
0.7
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
RIP Kinase
RIPK1
Pathway
Apoptosis
NF-κB
Source data