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Compound Detail

CHEMBL162946

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CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cncc3C)CC2)CC1

Basic Information

ChEMBL ID CHEMBL162946
Phase Preclinical
Structure Type MOL
InChI Key KBSCLJAQJYVUQQ-GKPLWNPISA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

541.5
MW (Da)
5.61
ALogP
5
HBA
0
HBD
58.0
PSA (Ų)
0.35
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H37BrN4O2
MW 541.53
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.66

Activity Summary

Ki 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 5
CHEMBL274
Ki 7.64 7.64 23.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1300.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 5 Ki = 23.0 nM 7.64 Inhibition of [125I]RANTES binding to CCR5 receptor. 12639564

Literature References

PubMed DOI Target Context # Activities
12639564 10.1016/s0960-894x(02)01063-6 C-C chemokine receptor type 5 1
12639564 10.1016/s0960-894x(02)01063-6 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine