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Compound Detail

CHEMBL1924047

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C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1

Basic Information

ChEMBL ID CHEMBL1924047
Phase Preclinical
Structure Type MOL
InChI Key DVEKJMIGSBNUCB-YXWZOGTMSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
7
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
4.78
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.45
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 C29H39N2O2+
MW 447.64
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.10

Activity Summary

Kd 1 meas. best 10.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 10.3 10.3 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 85.0 mL.min-1.g-1 Homo sapiens
CL 76.0 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 85.0 mL.min-1.g-1 Homo sapiens
T1/2 8.8 hr Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Kd = 0.05012 nM 10.3 Antagonist potency at M3 receptor in Dunkin Hartley guinea pig trachea assessed ... 22047691

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 5
22047691 10.1016/j.bmcl.2011.10.002 ADMET 2
22047691 10.1016/j.bmcl.2011.10.002 Cavia porcellus 2
22047691 10.1016/j.bmcl.2011.10.002 Unchecked 1
22047691 10.1016/j.bmcl.2011.10.002 Plasma 1
22047691 10.1016/j.bmcl.2011.10.002 Liver microsomes 1
22047691 10.1016/j.bmcl.2011.10.002 Muscarinic acetylcholine receptor M3 1

Data from ChEMBL 36 via Core Engine