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Compound Detail

CHEMBL4579623

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[3H]CC([3H])C(=O)NCCCCNC(=O)NC(=N)NCCC[C@H](N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)[C@@H](C)CC

Basic Information

ChEMBL ID CHEMBL4579623
Phase Preclinical
Structure Type MOL
InChI Key WNFLQFAPYRIZST-JVWVBCIYSA-N
Parent Compound CHEMBL3787706
Active Moiety CHEMBL3787706
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

987.2
MW (Da)
-0.67
ALogP
11
HBA
14
HBD
390.8
PSA (Ų)
0.03
QED
3
Ro5 Violations
30
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H78N14O10
MW 991.23
Aromatic Rings 1
Heavy Atoms 70
NP-Likeness 0.05

Activity Summary

Ki 1 meas. best 9.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL4123
Ki 9.29 9.29 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neurotensin receptor type 1 Ki = 0.51 nM 9.29 Binding affinity to human neurotensin receptor 1 31938457

Literature References

PubMed DOI Target Context # Activities
31938457 10.1021/acsmedchemlett.9b00462 Neurotensin receptor type 1 1

Data from ChEMBL 36 via Core Engine