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Compound Detail

CHEMBL395493

SPINORPHIN
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CC(C)C[C@H](N)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)O)[C@@H](C)O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL395493
Name SPINORPHIN
Phase Preclinical
Structure Type BOTH
InChI Key BXIFNVGZIMFBQB-DYDSHOKNSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

877.0
MW (Da)
1.22
ALogP
10
HBA
10
HBD
285.4
PSA (Ų)
0.07
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H64N8O10
MW 877.05
Aromatic Rings 3
Heavy Atoms 63
NP-Likeness 0.06

Activity Summary

IC50 2 meas. best 10.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 10.32 10.32 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 0.0481 nM 10.32 Antagonist activity at human recombinant P2X3 receptor expressed in Xenopus oocy... 17676725

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 Fibroblast 10
- 10.6019/CHEMBL5303304 U2OS 9
17676725 10.1021/jm070114m P2X purinoceptor 3 3
- 10.6019/CHEMBL5303304 HEK-293T 3
17676725 10.1021/jm070114m P2X purinoceptor 1 1
17676725 10.1021/jm070114m P2X purinoceptor 7 1
- 10.6019/CHEMBL5665443 Methyl-CpG-binding domain protein 4 1
- 10.6019/CHEMBL5665443 DNA-3-methyladenine glycosylase 1
- 10.6019/CHEMBL5665443 Adenine DNA glycosylase 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 1 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 2 1
- 10.6019/CHEMBL5665443 Endonuclease III-like protein 1 1
- 10.6019/CHEMBL5665443 N-glycosylase/DNA lyase 1
- 10.6019/CHEMBL5665443 Single-strand selective monofunctional uracil DNA glycosylase 1
- 10.6019/CHEMBL5665443 G/T mismatch-specific thymine DNA glycosylase 1
- 10.6019/CHEMBL5665443 Uracil-DNA glycosylase 1

Data from ChEMBL 36 via Core Engine