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Compound Detail

CHEMBL3099947

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O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)NC1CC1

Basic Information

ChEMBL ID CHEMBL3099947
Phase Preclinical
Structure Type MOL
InChI Key PYPUGVATTLSFNC-FQEVSTJZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

471.5
MW (Da)
3.02
ALogP
6
HBA
4
HBD
103.3
PSA (Ų)
0.46
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 C25H30FN3O5
MW 471.53
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.01

Activity Summary

IC50 3 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 1
CHEMBL2413
IC50 9.2 9.2 0.6 1
C-C chemokine receptor type 1
CHEMBL5499
IC50 7.0 7.0 101.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.42 5.42 3800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24332486 10.1016/j.bmcl.2013.11.062 C-C chemokine receptor type 1 2
24332486 10.1016/j.bmcl.2013.11.062 Voltage-gated inwardly rectifying potassium channel KCNH2 1
24332486 10.1016/j.bmcl.2013.11.062 Caco-2 1
24332486 10.1016/j.bmcl.2013.11.062 Hepatocyte 1
24332486 10.1016/j.bmcl.2013.11.062 Liver microsome 1

Data from ChEMBL 36 via Core Engine