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Compound Detail

CHEMBL271750

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CC1(N2CCC(c3cc(-c4ccc(F)cc4Cl)c4c(c3)N(c3c(Cl)cccc3Cl)C(=O)NC4)CC2)CC1

Basic Information

ChEMBL ID CHEMBL271750
Phase Preclinical
Structure Type MOL
InChI Key BCCKAGLVBBEKGJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

558.9
MW (Da)
8.55
ALogP
2
HBA
1
HBD
35.6
PSA (Ų)
0.35
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27Cl3FN3O
MW 558.91
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.41

Activity Summary

IC50 1 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Blood
CHEMBL613416
IC50 8.12 8.12 7.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 83.84 ng.hr.mL-1 Rattus norvegicus
CL 50.9 mL.min-1.kg-1 Rattus norvegicus
F 22.6 % Rattus norvegicus
T1/2 1.9 hr Rattus norvegicus
Vd 6.3 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Blood IC50 = 7.6 nM 8.12 Suppression of TNFalpha production in LPS-stimulated whole blood 18271520

Literature References

PubMed DOI Target Context # Activities
18271520 10.1021/jm070654j Rattus norvegicus 5
18271520 10.1021/jm070654j Blood 1

Data from ChEMBL 36 via Core Engine