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Assay Detail

CHEMBL5737050

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Binding
fluorescence anisotropy assay: The affinity of Example 1-33 for galectins were determined by a fluorescence anisotropy assay where the compound was used as an inhibitor of the interaction between galectin and a fluorescein tagged saccharide probe as described Sörme, P., Kahl-Knutsson, B., Huflejt, M., Nilsson, U. J., and Leffler H. (2004) Fluorescence polarization as an analytical tool to evaluate galectin-ligand interactions. Anal. Biochem. 334: 36-47, (Sörme et al., 2004) and Monovalent interactions of Galectin-1 By Salomonsson, Emma; Larumbe, Amaia; Tejler, Johan; Tullberg, Erik; Rydberg, Hanna; Sundin, Anders; Khabut, Areej; Frejd, Torbjorn; Lobsanov, Yuri D.; Rini, James M.; et al, From Biochemistry (2010), 49(44), 9518-9532, (Salomonsson et al., 2010).
78
Total Activities
26
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Galectin-3 (CHEMBL4531)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Galactoside inhibitor of galectins
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 26 5.74 7.16
kon 26 - -
k_off 26 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5849127 3 7.16
CHEMBL5746410 3 6.70
CHEMBL5837954 3 6.66
CHEMBL5859811 3 6.60
CHEMBL5777987 3 6.60
CHEMBL5871228 3 6.38
CHEMBL5850132 3 6.24
CHEMBL5807477 3 5.85
CHEMBL5954468 3 5.77
CHEMBL5993674 3 5.77
CHEMBL5978139 3 5.68
CHEMBL5866001 3 5.66
CHEMBL5950915 3 5.58
CHEMBL5890322 3 5.55
CHEMBL5829222 3 5.55
CHEMBL5790628 3 5.51
CHEMBL5772323 3 5.34
CHEMBL5925466 3 5.34
CHEMBL5929368 3 5.24
CHEMBL5809155 3 5.22
CHEMBL5966583 3 5.22
CHEMBL5865693 3 5.19
CHEMBL5887621 3 5.18
CHEMBL5809066 3 5.10
CHEMBL5858997 3 5.07
CHEMBL5921738 3 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5849127 Kd = 69.0 nM 7.16
CHEMBL5746410 Kd = 200.0 nM 6.70
CHEMBL5837954 Kd = 220.0 nM 6.66
CHEMBL5777987 Kd = 250.0 nM 6.60
CHEMBL5859811 Kd = 250.0 nM 6.60
CHEMBL5871228 Kd = 420.0 nM 6.38
CHEMBL5850132 Kd = 580.0 nM 6.24
CHEMBL5807477 Kd = 1400.0 nM 5.85
CHEMBL5954468 Kd = 1700.0 nM 5.77
CHEMBL5993674 Kd = 1700.0 nM 5.77
CHEMBL5978139 Kd = 2100.0 nM 5.68
CHEMBL5866001 Kd = 2200.0 nM 5.66
CHEMBL5950915 Kd = 2600.0 nM 5.58
CHEMBL5890322 Kd = 2800.0 nM 5.55
CHEMBL5829222 Kd = 2800.0 nM 5.55
CHEMBL5790628 Kd = 3100.0 nM 5.51
CHEMBL5925466 Kd = 4600.0 nM 5.34
CHEMBL5772323 Kd = 4600.0 nM 5.34
CHEMBL5929368 Kd = 5700.0 nM 5.24
CHEMBL5966583 Kd = 6000.0 nM 5.22
CHEMBL5809155 Kd = 6000.0 nM 5.22
CHEMBL5865693 Kd = 6500.0 nM 5.19
CHEMBL5887621 Kd = 6600.0 nM 5.18
CHEMBL5809066 Kd = 8000.0 nM 5.10
CHEMBL5858997 Kd = 8600.0 nM 5.07
CHEMBL5921738 Kd = 9700.0 nM 5.01
CHEMBL5929368 kon = - -
CHEMBL5777987 k_off = - s-1 -
CHEMBL5777987 kon = - -
CHEMBL5993674 k_off = - s-1 -
CHEMBL5954468 kon = - -
CHEMBL5978139 k_off = - s-1 -
CHEMBL5978139 kon = - -
CHEMBL5925466 k_off = - s-1 -
CHEMBL5925466 kon = - -
CHEMBL5849127 k_off = - s-1 -
CHEMBL5849127 kon = - -
CHEMBL5929368 k_off = - s-1 -
CHEMBL5772323 k_off = - s-1 -
CHEMBL5887621 k_off = - s-1 -
CHEMBL5887621 kon = - -
CHEMBL5865693 k_off = - s-1 -
CHEMBL5865693 kon = - -
CHEMBL5790628 k_off = - s-1 -
CHEMBL5809155 k_off = - s-1 -
CHEMBL5954468 k_off = - s-1 -
CHEMBL5790628 kon = - -
CHEMBL5772323 kon = - -
CHEMBL5966583 kon = - -
CHEMBL5966583 k_off = - s-1 -