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Compound Detail

CHEMBL5561817

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Nc1n[nH]c(=O)c2c1c(-c1ccc3c(c1)CCN3C(=O)Cc1cccc(OC(F)(F)F)c1)nn2CCC1CNC1

Basic Information

ChEMBL ID CHEMBL5561817
Phase Preclinical
Structure Type MOL
InChI Key HJYUFPSFSUFGIK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

553.5
MW (Da)
3.01
ALogP
8
HBA
3
HBD
131.2
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26F3N7O3
MW 553.55
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.29

Activity Summary

EC50 1 meas. best 6.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L929
CHEMBL612267
EC50 6.44 6.44 365.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 13.8 mL.min-1.g-1 Homo sapiens
T1/2 1.674 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
L929 EC50 = 365.8 nM 6.44 Anti-necroptosis activity against TSZ-induced mouse L929 cells 38171150

Literature References

PubMed DOI Target Context # Activities
38171150 10.1016/j.ejmech.2023.116076 ADMET 2
38171150 10.1016/j.ejmech.2023.116076 Receptor-interacting serine/threonine-protein kinase 1 1
38171150 10.1016/j.ejmech.2023.116076 HT-29 1
38171150 10.1016/j.ejmech.2023.116076 U-937 1
38171150 10.1016/j.ejmech.2023.116076 L929 1

Data from ChEMBL 36 via Core Engine