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Compound Detail

CHEMBL273915

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COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC

Basic Information

ChEMBL ID CHEMBL273915
Phase Preclinical
Structure Type MOL
InChI Key SGSDMASCYPMWHE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

790.9
MW (Da)
6.59
ALogP
11
HBA
1
HBD
141.9
PSA (Ų)
0.11
QED
3
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H50N4O9
MW 790.91
Aromatic Rings 5
Heavy Atoms 58
NP-Likeness -0.61

Activity Summary

IC50 2 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
IC50 8.34 8.34 4.6 1
Substance-P receptor
CHEMBL3942
IC50 8.15 8.15 7.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 4.56 nM 8.34 Antagonistic activity against histamine H1 receptor -
Substance-P receptor IC50 = 7.0 nM 8.15 Antagonistic activity against Tachykinin receptor 1 -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10098-1 Substance-P receptor 1
- 10.1016/S0960-894X(97)10098-1 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine