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Compound Detail

CHEMBL95243

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COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccc(OC)c(OC)c5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL95243
Phase Preclinical
Structure Type MOL
InChI Key RBJZEZVXAVEQFQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

804.9
MW (Da)
6.68
ALogP
12
HBA
0
HBD
130.9
PSA (Ų)
0.08
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 C46H52N4O9
MW 804.94
Aromatic Rings 5
Heavy Atoms 59
NP-Likeness -0.64

Activity Summary

IC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
IC50 8.22 8.22 6.0 1
Substance-P receptor
CHEMBL3942
IC50 8.12 8.12 7.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 6.02 nM 8.22 Antagonistic activity against histamine H1 receptor -
Substance-P receptor IC50 = 7.63 nM 8.12 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