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Assay Detail

CHEMBL4022510

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiinflammatory activity in primary human endothelial keratinocytes assessed as inhibition of IL-17A/TNF-alpha induced IL-8 production preincubated for 2 hrs followed by cytokine addition measured after 72 hrs by HTRF assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Keratinocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Keratinocyte (CHEMBL613995)
Type CELL-LINE

Publication

The design, synthesis, and anti-inflammatory evaluation of a drug-like library based on the natural product valerenic acid.
Egbewande FA, Nilsson N, White JM, Coster MJ, Davis RA.
Bioorg Med Chem Lett (2017) 27 : 3185 -3189
PubMed 28558967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.32 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088435 1 5.55
CHEMBL4072446 1 5.54
CHEMBL4067177 1 5.33
CHEMBL4080571 1 5.31
CHEMBL4102786 1 5.12
CHEMBL4099378 1 5.08
CHEMBL4096155 1 -
CHEMBL4085993 1 -
CHEMBL4103910 1 -
CHEMBL4104798 1 -
CHEMBL4078502 1 -
CHEMBL1545045 VALERENIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088435 IC50 = 2800.0 nM 5.55
CHEMBL4072446 IC50 = 2900.0 nM 5.54
CHEMBL4067177 IC50 = 4700.0 nM 5.33
CHEMBL4080571 IC50 = 4900.0 nM 5.31
CHEMBL4102786 IC50 = 7500.0 nM 5.12
CHEMBL4099378 IC50 = 8300.0 nM 5.08
CHEMBL4096155 IC50 - -
CHEMBL4085993 IC50 - -
CHEMBL4103910 IC50 - -
CHEMBL4104798 IC50 - -
CHEMBL4078502 IC50 - -
CHEMBL1545045 VALERENIC ACID IC50 - -