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Compound Detail

CHEMBL1807823

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O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3)c2s1

Basic Information

ChEMBL ID CHEMBL1807823
Phase Preclinical
Structure Type MOL
InChI Key FMRMQJKRHKYSLD-IBGZPJMESA-N
3
Targets
3
Activities
2
Assay Types
4
PK Parameters
8
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
2.87
ALogP
7
HBA
5
HBD
97.4
PSA (Ų)
0.26
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29N3O3S2
MW 447.63
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.43

Activity Summary

IC50 2 meas. best 6.6
EC50 1 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 9.1 9.1 0.8 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 6.6 6.6 251.2 1
D(2) dopamine receptor
CHEMBL217
IC50 5.4 5.4 3981.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.0 mL.min-1.g-1 Homo sapiens
CL 9.0 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 3.0 uL.min-1.(10^6cells)-1 Homo sapiens
T1/2 10.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 6
21723724 10.1016/j.bmcl.2011.05.097 Beta-1 adrenergic receptor 2
21723724 10.1016/j.bmcl.2011.05.097 Unchecked 2
21723724 10.1016/j.bmcl.2011.05.097 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL3301361 No relevant target 2
21723724 10.1016/j.bmcl.2011.05.097 D(2) dopamine receptor 1
21723724 10.1016/j.bmcl.2011.05.097 Rattus norvegicus 1
21723724 10.1016/j.bmcl.2011.05.097 No relevant target 1

Data from ChEMBL 36 via Core Engine