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Compound Detail

CHEMBL542908

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COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC.Cl

Basic Information

ChEMBL ID CHEMBL542908
Phase Preclinical
Structure Type MOL
InChI Key YFWUUKSPYPKQPB-UHFFFAOYSA-N
Parent Compound CHEMBL1191766
Active Moiety CHEMBL1191766
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

774.9
MW (Da)
7.00
ALogP
10
HBA
1
HBD
132.7
PSA (Ų)
0.08
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H51ClN4O8
MW 811.38
Aromatic Rings 5
Heavy Atoms 57
NP-Likeness -0.70

Activity Summary

IC50 2 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL3942
IC50 7.57 7.57 27.0 1
Histamine H1 receptor
CHEMBL231
IC50 5.03 5.03 9447.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 27.0 nM 7.57 Antagonism of the guinea pig tachykinin NK1 receptor -
Histamine H1 receptor IC50 = 9447.0 nM 5.03 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