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Compound Detail

CHEMBL143156

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O=C(CN1CCCC1)N1CCC(COCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL143156
Phase Preclinical
Structure Type MOL
InChI Key ABRLODMDKOBAGA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

528.5
MW (Da)
5.90
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.42
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30F6N2O2
MW 528.54
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.94

Activity Summary

IC50 1 meas. best 9.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.62 9.62 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 26.0 mL.min-1.kg-1 Cavia porcellus
Cmax 2.0 hr Cavia porcellus
F 48.0 % Cavia porcellus
T1/2 7.0 hr Cavia porcellus
Vss 12.0 kg-1 Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.24 nM 9.62 Binding affinity at human tachykinin receptor 1 by measuring its ability to disp... 9804702

Literature References

PubMed DOI Target Context # Activities
9804702 10.1021/jm980376b Cavia porcellus 4
9804702 10.1021/jm980376b Substance-P receptor 2
9804702 10.1021/jm980376b ADMET 1

Data from ChEMBL 36 via Core Engine