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Compound Detail

CHEMBL96466

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O=C(c1nc2ccccc2n1Cc1ccc(F)cc1)C1CCN(CCC2(c3ccc4c(c3)OCO4)CCN(C(=O)c3ccc(Cl)cc3Cl)C2)CC1

Basic Information

ChEMBL ID CHEMBL96466
Phase Preclinical
Structure Type MOL
InChI Key QPFYLKDZMPQIPZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

727.7
MW (Da)
8.03
ALogP
7
HBA
0
HBD
76.9
PSA (Ų)
0.14
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H37Cl2FN4O4
MW 727.66
Aromatic Rings 5
Heavy Atoms 51
NP-Likeness -1.17

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL3942
IC50 8.3 8.3 5.0 1
Histamine H1 receptor
CHEMBL231
IC50 8.16 8.16 6.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 5.0 nM 8.3 Antagonistic activity against Tachykinin receptor 1 -
Histamine H1 receptor IC50 = 6.89 nM 8.16 Antagonistic activity against histamine H1 receptor -

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