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Compound Detail

CHEMBL4172635

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COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl

Basic Information

ChEMBL ID CHEMBL4172635
Phase Preclinical
Structure Type MOL
InChI Key NWSUDJQTTGDPIR-UHFFFAOYSA-N
4
Targets
7
Activities
1
Assay Types
6
PK Parameters
14
Publications
0
Known Names

Molecular Properties

352.2
MW (Da)
2.73
ALogP
5
HBA
1
HBD
81.2
PSA (Ų)
0.92
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H8Cl2FN3O3S
MW 352.17
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -2.00

Activity Summary

IC50 7 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 4
CHEMBL5410
IC50 9.0 9.0 1.0 1
Unchecked
CHEMBL612545
IC50 9.0 9.0 1.0 1
C-C chemokine receptor type 4
CHEMBL2414
IC50 8.6 7.575 2.5 4
C-C chemokine receptor type 4
CHEMBL4295899
IC50 8.5 8.5 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.3 mL.min-1.kg-1 Rattus norvegicus
CL 3.7 mL.min-1.kg-1 Canis lupus familiaris
F 100.0 % Rattus norvegicus
F 100.0 % Canis lupus familiaris
T1/2 2.5 hr Rattus norvegicus
T1/2 0.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 4 7
28947948 10.1021/acsmedchemlett.7b00315 Rattus norvegicus 4
28947948 10.1021/acsmedchemlett.7b00315 Canis familiaris 4
28947948 10.1021/acsmedchemlett.7b00315 No relevant target 3
28947948 10.1021/acsmedchemlett.7b00315 ADMET 1
28947948 10.1021/acsmedchemlett.7b00315 Hepatocyte 1
28947948 10.1021/acsmedchemlett.7b00315 Unchecked 1
28947948 10.1021/acsmedchemlett.7b00315 C-X-C chemokine receptor type 1 1
28947948 10.1021/acsmedchemlett.7b00315 C-X-C chemokine receptor type 2 1
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 1 1
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 2 1
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 5 1
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 7 1
28947948 10.1021/acsmedchemlett.7b00315 C-C chemokine receptor type 8 1

Data from ChEMBL 36 via Core Engine