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Compound Detail

CHEMBL68800

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COc1cc(OC2CCN([C@H]3CCCc4c3ccc[n+]4[O-])CC2)c(F)cc1C(=O)N1CCC(N2C(=O)OCc3ccccc32)CC1

Basic Information

ChEMBL ID CHEMBL68800
Phase Preclinical
Structure Type MOL
InChI Key XMCRJVIWAZBDSM-PMERELPUSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

630.7
MW (Da)
5.15
ALogP
7
HBA
0
HBD
98.5
PSA (Ų)
0.27
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H39FN4O6
MW 630.72
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.52

Activity Summary

Ki 2 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 8.77 8.77 1.7 1
Oxytocin receptor
CHEMBL3996
Ki 8.07 8.07 8.5 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 13159.56 nM Rattus norvegicus
Cmax 10939.88 nM Rattus norvegicus
F 65.0 % Rattus norvegicus
T1/2 1.9 hr Rattus norvegicus
T1/2 0.95 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9622556 10.1021/jm9800797 Rattus norvegicus 6
9622556 10.1021/jm9800797 Oxytocin receptor 2
9622556 10.1021/jm9800797 ADMET 1

Data from ChEMBL 36 via Core Engine