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Compound Detail

CHEMBL24646

PIMOBENDAN
🧪 Phase II
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🧪 Phase II
COc1ccc(-c2nc3cc(C4=NNC(=O)CC4C)ccc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL24646
Name PIMOBENDAN
Phase Phase II
Structure Type MOL
InChI Key GLBJJMFZWDBELO-UHFFFAOYSA-N

Known Names

Acardi Dl-pimobendan Pimobendan Pimobendan component of fortekor plus Pimobendane Racemic pimobendan UD-CG-115 UD-CG-115BS UDCG-115 Vetmedin
5
Targets
9
Activities
2
Assay Types
5
PK Parameters
20
Publications
10
Known Names

Molecular Properties

334.4
MW (Da)
3.10
ALogP
4
HBA
2
HBD
79.4
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic
USAN Stem -dan
USAN Year 1990

Extended Properties

Molecular Formula C19H18N4O2
MW 334.38
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.70

Activity Summary

IC50 6 meas. best 6.39
EC50 3 meas. best 5.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 3
CHEMBL2094125
IC50 6.39 5.555 410.0 2
Unchecked
CHEMBL612545
IC50 5.54 5.3133 2892.1 3
Aorta
CHEMBL613606
EC50 5.33 5.33 4670.0 1
Type-1 angiotensin II receptor
CHEMBL3374
IC50 4.77 4.77 17000.0 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.kg-1 Homo sapiens
CL 14.0 mL.min-1.g-1 Homo sapiens
Fu 0.024 - Homo sapiens
MRT 2.2 hr Homo sapiens
T1/2 1.8 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1007/s00044-011-9835-6 Sus scrofa 5
2544724 10.1021/jm00127a015 Canis familiaris 5
30523084 10.1126/science.aat9446 Plasmodium berghei 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
18426954 10.1124/dmd.108.020479 ADMET 4
20451399 10.1016/j.bmc.2010.04.027 Aorta 4
- 10.6019/CHEMBL4808148 Histone deacetylase 6 3
37468498 10.1038/s41467-023-40064-9 Androgen receptor 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
30523084 10.1126/science.aat9446 HepG2-CD81 2
- 10.6019/CHEMBL3301361 ADMET 2
37468498 10.1038/s41467-023-40064-9 Beta-1 adrenergic receptor 2
2213839 10.1021/jm00172a031 Rattus norvegicus 2
2544724 10.1021/jm00127a015 Felis catus 2
2544724 10.1021/jm00127a015 Rattus norvegicus 2
- 10.1016/S0960-894X(01)80288-2 Phosphodiesterase 3 2
- 10.1016/S0960-894X(01)80288-2 NON-PROTEIN TARGET 2
37468498 10.1038/s41467-023-40064-9 Beta-2 adrenergic receptor 2
3027335 10.1021/jm00385a001 Phosphodiesterase; PDE3 & PDE4 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2

Data from ChEMBL 36 via Core Engine