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Compound Detail

CHEMBL4062686

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Cc1c(COc2cc(F)c(CNC[C@@H](O)CC(=O)O)cc2F)cccc1-c1ccc2c(c1)OCCO2

Basic Information

ChEMBL ID CHEMBL4062686
Phase Preclinical
Structure Type MOL
InChI Key UUBRFEROHJGRBO-FQEVSTJZSA-N
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

499.5
MW (Da)
4.22
ALogP
6
HBA
3
HBD
97.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27F2NO6
MW 499.51
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.53

Activity Summary

IC50 6 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Programmed cell death 1 ligand 1
CHEMBL3580522
IC50 7.1 7.1 80.0 3
Programmed cell death protein 1/Programmed cell death 1 ligand 1
CHEMBL4523993
IC50 7.1 7.1 80.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28613862 10.1021/acs.jmedchem.7b00293 Programmed cell death 1 ligand 1 6
30020783 10.1021/acs.jmedchem.8b00541 Programmed cell death 1 ligand 1 1
30384043 10.1016/j.ejmech.2018.10.044 Programmed cell death 1 ligand 1 1
33517226 10.1016/j.bmc.2021.116038 Programmed cell death protein 1/Programmed cell death 1 ligand 1 1
33272783 10.1016/j.ejmech.2020.113001 Programmed cell death protein 1/Programmed cell death 1 ligand 1 1
31761384 10.1016/j.ejmech.2019.111876 Programmed cell death protein 1/Programmed cell death 1 ligand 1 1

Data from ChEMBL 36 via Core Engine