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Compound Detail

CHEMBL1172625

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C=CCN(C(=O)Cc1ccc(S(=O)(=O)NC)cc1)C1CCN(C[C@H]2CN(C(=O)C3CCCC3)C[C@]2(O)c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL1172625
Phase Preclinical
Structure Type MOL
InChI Key XPFKJEFRGMJTEE-DODOAAEWSA-N
2
Targets
2
Activities
2
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

622.8
MW (Da)
3.15
ALogP
6
HBA
2
HBD
110.3
PSA (Ų)
0.37
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H46N4O5S
MW 622.83
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -1.14

Activity Summary

EC50 1 meas. best 9.1
IC50 1 meas. best 8.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 9.1 9.1 0.8 1
C-C chemokine receptor type 5
CHEMBL274
IC50 8.81 8.81 1.5 1

Pharmacokinetic Data

Parameter Value Units Species
CL 121.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 2252.62 nM Rattus norvegicus
F 1.7 % Rattus norvegicus
T1/2 0.77 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20561788 10.1016/j.bmcl.2010.05.102 Rattus norvegicus 5
20561788 10.1016/j.bmcl.2010.05.102 Human immunodeficiency virus 1 4
20561788 10.1016/j.bmcl.2010.05.102 Voltage-gated inwardly rectifying potassium channel KCNH2 2
20561788 10.1016/j.bmcl.2010.05.102 Caco-2 2
20561788 10.1016/j.bmcl.2010.05.102 C-C chemokine receptor type 5 1
20561788 10.1016/j.bmcl.2010.05.102 ADMET 1

Data from ChEMBL 36 via Core Engine