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Compound Detail

CHEMBL3765335

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C[C@@H](C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)n1ncccc1=O

Basic Information

ChEMBL ID CHEMBL3765335
Phase Preclinical
Structure Type MOL
InChI Key PBXGYXYBIGMVQD-KBABAZTHSA-N
5
Targets
8
Activities
2
Assay Types
19
PK Parameters
18
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
2.84
ALogP
6
HBA
3
HBD
96.2
PSA (Ų)
0.53
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28N4O3
MW 432.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.57

Activity Summary

EC50 7 meas. best 8.68
IC50 1 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 8.68 8.625 2.1 2
Beta-3 adrenergic receptor
CHEMBL3124732
EC50 8.6 8.26 2.5 2
Beta-3 adrenergic receptor
CHEMBL4400
EC50 7.41 7.41 39.0 1
Beta-3 adrenergic receptor
CHEMBL4031
EC50 6.61 6.445 245.0 2
Unchecked
CHEMBL612545
IC50 5.64 5.64 2300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 36.0 mL.min-1.kg-1 Rattus norvegicus
CL 23.0 mL.min-1.kg-1 Canis lupus familiaris
CL 33.0 mL.min-1.kg-1 Macaca mulatta
CL 180.0 mL.min-1.kg-1 Rattus norvegicus
CL 59.0 mL.min-1.kg-1 Canis lupus familiaris
CL 46.0 mL.min-1.kg-1 Macaca mulatta
CL 10.0 mL.min-1.kg-1 Homo sapiens
CL 31.0 mL.min-1.kg-1 Rattus norvegicus
CL 34.0 mL.min-1.kg-1 Canis lupus familiaris
CL 17.0 mL.min-1.kg-1 Macaca mulatta
F 10.0 % Rattus norvegicus
F 91.0 % Canis lupus familiaris
F 29.0 % Macaca mulatta
Fu 0.2 - Rattus norvegicus
Fu 0.39 - Canis lupus familiaris
Fu 0.71 - Macaca mulatta
T1/2 2.0 hr Rattus norvegicus
T1/2 9.0 hr Canis lupus familiaris
T1/2 9.0 hr Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26709102 10.1021/acs.jmedchem.5b01372 Beta-3 adrenergic receptor 13
26709102 10.1021/acs.jmedchem.5b01372 Rattus norvegicus 8
26709102 10.1021/acs.jmedchem.5b01372 Rhesus monkey 6
26709102 10.1021/acs.jmedchem.5b01372 Canis familiaris 6
26709102 10.1021/acs.jmedchem.5b01372 Plasma 4
26709102 10.1021/acs.jmedchem.5b01372 Liver microsome 3
26709102 10.1021/acs.jmedchem.5b01372 NON-PROTEIN TARGET 3
26709102 10.1021/acs.jmedchem.5b01372 Unchecked 2
26709102 10.1021/acs.jmedchem.5b01372 UDP-glucuronosyltransferase 2B9 1
26709102 10.1021/acs.jmedchem.5b01372 ADMET 1
26709102 10.1021/acs.jmedchem.5b01372 HepG2 1
26709102 10.1021/acs.jmedchem.5b01372 Sodium-dependent serotonin transporter 1
26709102 10.1021/acs.jmedchem.5b01372 No relevant target 1
26709102 10.1021/acs.jmedchem.5b01372 Sodium channel protein type 5 subunit alpha 1
26709102 10.1021/acs.jmedchem.5b01372 Voltage-dependent L-type calcium channel subunit alpha-1C 1
26709102 10.1021/acs.jmedchem.5b01372 Voltage-gated inwardly rectifying potassium channel KCNH2 1
26709102 10.1021/acs.jmedchem.5b01372 Beta-2 adrenergic receptor 1
26709102 10.1021/acs.jmedchem.5b01372 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine