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Compound Detail

CHEMBL4638345

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CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C(=O)CC[C@H](N)C(=O)O)CC2)cc1

Basic Information

ChEMBL ID CHEMBL4638345
Phase Preclinical
Structure Type MOL
InChI Key KZROHPAQERRFBQ-SANMLTNESA-N
6
Targets
6
Activities
1
Assay Types
4
PK Parameters
18
Publications
0
Known Names

Molecular Properties

542.6
MW (Da)
3.76
ALogP
5
HBA
3
HBD
125.2
PSA (Ų)
0.38
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39FN4O5
MW 542.65
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -1.21

Activity Summary

IC50 6 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 8.08 8.08 8.3 1
NIH3T3
CHEMBL614822
IC50 4.74 4.74 18200.0 1
CHO-K1
CHEMBL614031
IC50 4.29 4.29 51000.0 1
Vero
CHEMBL391
IC50 4.26 4.26 54700.0 1
HFL1
CHEMBL612547
IC50 4.26 4.26 55200.0 1
L929
CHEMBL612267
IC50 4.19 4.19 64000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1910.0 ng.hr.mL-1 Rattus norvegicus
AUC 2030.0 ng.hr.mL-1 Rattus norvegicus
CL 41.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 16.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32285676 10.1021/acs.jmedchem.0c00002 Mus musculus 12
32285676 10.1021/acs.jmedchem.0c00002 ADMET 10
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 2A 3
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 1A 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 7 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 6 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 4 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 3A 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 2C 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 2B 1
32285676 10.1021/acs.jmedchem.0c00002 5-hydroxytryptamine receptor 1B 1
32285676 10.1021/acs.jmedchem.0c00002 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32285676 10.1021/acs.jmedchem.0c00002 CHO-K1 1
32285676 10.1021/acs.jmedchem.0c00002 NIH3T3 1
32285676 10.1021/acs.jmedchem.0c00002 L929 1
32285676 10.1021/acs.jmedchem.0c00002 HFL1 1
32285676 10.1021/acs.jmedchem.0c00002 Vero 1
32285676 10.1021/acs.jmedchem.0c00002 No relevant target 1

Data from ChEMBL 36 via Core Engine