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Compound Detail

CHEMBL5572472

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Br.Cc1c(Nc2nccc3cc(CN4CC[C@@H](O)C4)cnc23)cccc1-c1cccc(-c2nc3ccc(CN4CC[C@@H](C(=O)O)C4)c(C#N)c3o2)c1C

Basic Information

ChEMBL ID CHEMBL5572472
Phase Preclinical
Structure Type MOL
InChI Key HZQVAVCVMDJMFN-GAQUOPITSA-N
Parent Compound CHEMBL6070227
Active Moiety CHEMBL6070227
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

693.8
MW (Da)
6.81
ALogP
10
HBA
3
HBD
151.6
PSA (Ų)
0.15
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H40BrN7O4
MW 774.72
Aromatic Rings 6
Heavy Atoms 52
NP-Likeness -0.93

Activity Summary

IC50 1 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Programmed cell death protein 1
CHEMBL3307223
IC50 8.51 8.51 3.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Programmed cell death protein 1 IC50 = 3.1 nM 8.51 Inhibition of human recombinant PD-1 by HTRF analysis 38348878

Literature References

PubMed DOI Target Context # Activities
38348878 10.1021/acs.jmedchem.3c02362 Programmed cell death protein 1 1

Data from ChEMBL 36 via Core Engine