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Assay Detail

CHEMBL803587

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Binding
In vitro potency against TNF alpha induced expression of Selectin E on human vascular endothelial cells using CAM ELISA assay
ChEMBL ↗
56
Total Activities
56
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 Expert

Target

E-selectin (CHEMBL3890) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.
Stewart AO, Bhatia PA, McCarty CM, Patel MV, Staeger MA, Arendsen DL, Gunawardana IW, Melcher LM, Zhu GD, Boyd SA, Fry DG, Cool BL, Kifle L, Lartey K, Marsh KC, Kempf-Grote AJ, Kilgannon P, Wisdom W, Meyer J, Gallatin WM, Okasinski GF.
J Med Chem (2001) 44 : 988 -1002
PubMed 11300880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.31 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266198 — — 1 8.30
CHEMBL268567 — — 1 7.92
CHEMBL267125 — — 1 7.89
CHEMBL267678 — — 1 7.70
CHEMBL267456 — — 1 7.70
CHEMBL269598 — — 1 7.50
CHEMBL6830 — — 1 7.37
CHEMBL6542 — — 1 7.36
CHEMBL269497 — — 1 7.35
CHEMBL6248 — — 1 7.30
CHEMBL262570 — — 1 7.26
CHEMBL6278 — — 1 7.26
CHEMBL6517 — — 1 7.22
CHEMBL269075 — — 1 7.06
CHEMBL6612 — — 1 7.00
CHEMBL263081 — — 1 6.89
CHEMBL266708 — — 1 6.85
CHEMBL266429 — — 1 6.82
CHEMBL6264 — — 1 6.70
CHEMBL268530 — — 1 6.70
CHEMBL6257 — — 1 6.60
CHEMBL269570 — — 1 6.47
CHEMBL6371 — — 1 6.30
CHEMBL267938 — — 1 6.22
CHEMBL428508 — — 1 6.21
CHEMBL263080 — — 1 6.18
CHEMBL6381 — — 1 6.16
CHEMBL6258 — — 1 5.82
CHEMBL266572 — — 1 5.77
CHEMBL266197 — — 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266198 — IC50 = 5.0 nM 8.30
CHEMBL268567 — IC50 = 12.0 nM 7.92
CHEMBL267125 — IC50 = 13.0 nM 7.89
CHEMBL267678 — IC50 = 20.0 nM 7.70
CHEMBL267456 — IC50 = 20.0 nM 7.70
CHEMBL269598 — IC50 = 32.0 nM 7.50
CHEMBL6830 — IC50 = 43.0 nM 7.37
CHEMBL6542 — IC50 = 44.0 nM 7.36
CHEMBL269497 — IC50 = 45.0 nM 7.35
CHEMBL6248 — IC50 = 50.0 nM 7.30
CHEMBL262570 — IC50 = 55.0 nM 7.26
CHEMBL6278 — IC50 = 55.0 nM 7.26
CHEMBL6517 — IC50 = 60.0 nM 7.22
CHEMBL269075 — IC50 = 88.0 nM 7.06
CHEMBL6612 — IC50 = 100.0 nM 7.00
CHEMBL263081 — IC50 = 130.0 nM 6.89
CHEMBL266708 — IC50 = 140.0 nM 6.85
CHEMBL266429 — IC50 = 150.0 nM 6.82
CHEMBL6264 — IC50 = 200.0 nM 6.70
CHEMBL268530 — IC50 = 200.0 nM 6.70
CHEMBL6257 — IC50 = 250.0 nM 6.60
CHEMBL269570 — IC50 = 340.0 nM 6.47
CHEMBL6371 — IC50 = 500.0 nM 6.30
CHEMBL267938 — IC50 = 600.0 nM 6.22
CHEMBL428508 — IC50 = 620.0 nM 6.21
CHEMBL263080 — IC50 = 660.0 nM 6.18
CHEMBL6381 — IC50 = 690.0 nM 6.16
CHEMBL6258 — IC50 = 1500.0 nM 5.82
CHEMBL266572 — IC50 = 1700.0 nM 5.77
CHEMBL266197 — IC50 = 1800.0 nM 5.75
CHEMBL266799 — IC50 = 2200.0 nM 5.66
CHEMBL6229 — IC50 = 3000.0 nM 5.52
CHEMBL6370 — IC50 = 3200.0 nM 5.50
CHEMBL267127 — IC50 = 4000.0 nM 5.40
CHEMBL6369 — IC50 = 8400.0 nM 5.08
CHEMBL268070 — IC50 = 15000.0 nM 4.82
CHEMBL267914 — IC50 = 16000.0 nM 4.80
CHEMBL6442 — IC50 = 17000.0 nM 4.77
CHEMBL6523 — IC50 = 22000.0 nM 4.66
CHEMBL269056 — IC50 = 27000.0 nM 4.57
CHEMBL269495 — IC50 = 42000.0 nM 4.38
CHEMBL6430 — IC50 = 49000.0 nM 4.31
CHEMBL266064 — IC50 = 95000.0 nM 4.02
CHEMBL6762 — IC50 > 4000.0 nM -
CHEMBL6316 — IC50 > 4000.0 nM -
CHEMBL6417 — IC50 > 100000.0 nM -
CHEMBL6249 — IC50 > 4000.0 nM -
CHEMBL6324 — IC50 > 4000.0 nM -
CHEMBL268667 — IC50 > 4000.0 nM -
CHEMBL268099 — IC50 > 1000.0 nM -