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Compound Detail

CHEMBL48981

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

Basic Information

ChEMBL ID CHEMBL48981
Phase Preclinical
Structure Type BOTH
InChI Key ORFISQWLBSTJAE-KTHKBMNISA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

660.8
MW (Da)
-0.06
ALogP
8
HBA
8
HBD
255.6
PSA (Ų)
0.06
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H52N8O7
MW 660.82
Aromatic Rings 1
Heavy Atoms 47
NP-Likeness 0.32

Activity Summary

Ki 2 meas. best 7.55
IC50 1 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL4123
IC50 7.72 7.72 19.0 1
Neurotensin receptor
CHEMBL2111438
Ki 7.55 7.55 28.0 1
Unchecked
CHEMBL612545
Ki 7.14 7.14 73.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7265123 10.1021/jm00136a004 Unchecked 3
- 10.1016/S0960-894X(00)80059-1 Unchecked 1
- 10.1016/S0960-894X(00)80059-1 Mus musculus 1
10743946 10.1016/s0960-894x(00)00018-4 Neurotensin receptor type 1 1
10579853 10.1021/jm9903444 Neurotensin receptor type 1 1
10498212 10.1016/s0960-894x(99)00420-5 Neurotensin receptor 1
915901 10.1021/jm00221a011 Rattus norvegicus 1
915901 10.1021/jm00221a011 Unchecked 1
915901 10.1021/jm00221a011 No relevant target 1

Data from ChEMBL 36 via Core Engine