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Assay Detail

CHEMBL818857

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

Binding
In vitro inhibitory potency compared to IL1-beta induced VCAM-1 in human endothelial cells (ELISA assay)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Endothelial cell
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Vascular cell adhesion protein 1 (CHEMBL3735)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides.
Zhu GD, Arendsen DL, Gunawardana IW, Boyd SA, Stewart AO, Fry DG, Cool BL, Kifle L, Schaefer V, Meuth J, Marsh KC, Kempf-Grote AJ, Kilgannon P, Gallatin WM, Okasinski GF.
J Med Chem (2001) 44 : 3469 -3487
PubMed 11585452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.93 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116070 1 8.15
CHEMBL117279 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116070 IC50 = 7.0 nM 8.15
CHEMBL117279 IC50 = 20.0 nM 7.70