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Compound Detail

CHEMBL1170627

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CC(C)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)CCCCN)C(C)(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL1170627
Phase Preclinical
Structure Type MOL
InChI Key ILBWCVGOOQVANC-FBDWWTLJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

788.0
MW (Da)
1.07
ALogP
9
HBA
10
HBD
282.2
PSA (Ų)
0.05
QED
2
Ro5 Violations
22
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H65N9O8
MW 788.00
Aromatic Rings 1
Heavy Atoms 56
NP-Likeness 0.39

Activity Summary

Kd 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL4123
Kd 8.24 8.24 5.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neurotensin receptor type 1 Kd = 5.71 nM 8.24 Binding affinity to human NTS1R assessed as dissociation constant 37094450

Literature References

PubMed DOI Target Context # Activities
20481538 10.1021/jm100092s Rattus norvegicus 2
37094450 10.1016/j.ejmech.2023.115386 Neurotensin receptor type 1 1

Data from ChEMBL 36 via Core Engine