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Compound Detail

CHEMBL30587

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O=C(c1ccc2oc(CN3CCC(n4cc(C(F)(F)F)ccc4=O)CC3)cc2c1)N1CCC(N2C(=O)OCc3ccccc32)CC1

Basic Information

ChEMBL ID CHEMBL30587
Phase Preclinical
Structure Type MOL
InChI Key HAOPKRIOLHXGOQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

634.7
MW (Da)
6.21
ALogP
7
HBA
0
HBD
88.2
PSA (Ų)
0.26
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H33F3N4O5
MW 634.66
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -0.95

Activity Summary

Ki 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 6.1 6.1 794.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 12000.0 ng.hr.mL-1 Rattus norvegicus
CL 6.0 mL.min-1.kg-1 Rattus norvegicus
F 79.0 % Rattus norvegicus
T1/2 1.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 794.33 nM 6.1 Displacement of 3[H]oxytocin from human oxytocin receptor 11992787

Literature References

PubMed DOI Target Context # Activities
11992787 10.1016/s0960-894x(02)00160-9 Rattus norvegicus 4
11992787 10.1016/s0960-894x(02)00160-9 Oxytocin receptor 2
11992787 10.1016/s0960-894x(02)00160-9 Albumin 1

Data from ChEMBL 36 via Core Engine