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Compound Detail

CHEMBL330430

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COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC.O=C(O)/C=C/C(=O)O

Basic Information

ChEMBL ID CHEMBL330430
Phase Preclinical
Structure Type MOL
InChI Key QJSGTTMHFKBELN-WLHGVMLRSA-N
Parent Compound CHEMBL97357
Active Moiety CHEMBL97357
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

773.7
MW (Da)
8.33
ALogP
8
HBA
0
HBD
86.1
PSA (Ų)
0.12
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H47Cl2FN4O9
MW 889.81
Aromatic Rings 5
Heavy Atoms 54
NP-Likeness -1.00

Activity Summary

IC50 2 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL3942
IC50 7.04 7.04 92.0 1
Histamine H1 receptor
CHEMBL231
IC50 6.91 6.91 124.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 92.0 nM 7.04 Antagonism of the guinea pig tachykinin NK1 receptor -
Histamine H1 receptor IC50 = 124.0 nM 6.91 Antagonism of the human histamine H1 receptor -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10097-X Histamine H1 receptor 1
- 10.1016/S0960-894X(97)10097-X Substance-P receptor 1

Data from ChEMBL 36 via Core Engine