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Compound Detail

CHEMBL427604

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CC[C@H](C)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCN)NC[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL427604
Phase Preclinical
Structure Type BOTH
InChI Key IXQSLTQEPOPVAT-KGAIBMCASA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

770.0
MW (Da)
1.88
ALogP
9
HBA
9
HBD
250.8
PSA (Ų)
0.07
QED
2
Ro5 Violations
25
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H67N9O6
MW 770.03
Aromatic Rings 2
Heavy Atoms 55
NP-Likeness 0.09

Activity Summary

EC50 1 meas. best 6.96
Ki 1 meas. best 10.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL3570
Ki 10.22 10.22 0.1 1
HT-29
CHEMBL384
EC50 6.96 6.96 110.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neurotensin receptor type 1 Ki = 0.06 nM 10.22 Binding affinity for Neurotensin Receptor -
HT-29 EC50 = 110.0 nM 6.96 Compound was tested in vitro to mobilize calcium from HT-29 cells -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00155-M Neurotensin receptor type 1 1
- 10.1016/0960-894X(95)00155-M HT-29 1
- 10.1016/0960-894X(95)00155-M Mus musculus 1

Data from ChEMBL 36 via Core Engine