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Assay Detail

CHEMBL5737049

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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).
ChEMBL ↗
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-1 (CHEMBL4915) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Galactoside inhibitor of galectins
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 26 7.21 8.22
kon 26 - -
k_off 26 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5866001 — — 3 8.22
CHEMBL5925466 — — 3 7.89
CHEMBL5829222 — — 3 7.72
CHEMBL5921738 — — 3 7.57
CHEMBL5890322 — — 3 7.55
CHEMBL5790628 — — 3 7.50
CHEMBL5950915 — — 3 7.48
CHEMBL5809066 — — 3 7.42
CHEMBL5978139 — — 3 7.36
CHEMBL5929368 — — 3 7.34
CHEMBL5772323 — — 3 7.30
CHEMBL5954468 — — 3 7.27
CHEMBL5809155 — — 3 7.25
CHEMBL5858997 — — 3 7.24
CHEMBL5966583 — — 3 7.20
CHEMBL5859811 — — 3 7.17
CHEMBL5865693 — — 3 7.15
CHEMBL5887621 — — 3 7.09
CHEMBL5746410 — — 3 7.07
CHEMBL5837954 — — 3 7.02
CHEMBL5871228 — — 3 7.02
CHEMBL5777987 — — 3 6.96
CHEMBL5850132 — — 3 6.80
CHEMBL5849127 — — 3 6.41
CHEMBL5807477 — — 3 6.31
CHEMBL5993674 — — 3 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5866001 — Kd = 6.0 nM 8.22
CHEMBL5925466 — Kd = 13.0 nM 7.89
CHEMBL5829222 — Kd = 19.0 nM 7.72
CHEMBL5921738 — Kd = 27.0 nM 7.57
CHEMBL5890322 — Kd = 28.0 nM 7.55
CHEMBL5790628 — Kd = 32.0 nM 7.50
CHEMBL5950915 — Kd = 33.0 nM 7.48
CHEMBL5809066 — Kd = 38.0 nM 7.42
CHEMBL5978139 — Kd = 44.0 nM 7.36
CHEMBL5929368 — Kd = 46.0 nM 7.34
CHEMBL5772323 — Kd = 50.0 nM 7.30
CHEMBL5954468 — Kd = 54.0 nM 7.27
CHEMBL5809155 — Kd = 56.0 nM 7.25
CHEMBL5858997 — Kd = 58.0 nM 7.24
CHEMBL5966583 — Kd = 63.0 nM 7.20
CHEMBL5859811 — Kd = 68.0 nM 7.17
CHEMBL5865693 — Kd = 71.0 nM 7.15
CHEMBL5887621 — Kd = 82.0 nM 7.09
CHEMBL5746410 — Kd = 85.0 nM 7.07
CHEMBL5837954 — Kd = 95.0 nM 7.02
CHEMBL5871228 — Kd = 95.0 nM 7.02
CHEMBL5777987 — Kd = 110.0 nM 6.96
CHEMBL5850132 — Kd = 160.0 nM 6.80
CHEMBL5849127 — Kd = 390.0 nM 6.41
CHEMBL5807477 — Kd = 490.0 nM 6.31
CHEMBL5993674 — Kd = 650.0 nM 6.19
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 — kon = - — -
CHEMBL5887621 — k_off = - s-1 -
CHEMBL5887621 — kon = - — -
CHEMBL5865693 — k_off = - s-1 -
CHEMBL5865693 — kon = - — -
CHEMBL5790628 — k_off = - s-1 -
CHEMBL5809155 — k_off = - s-1 -
CHEMBL5772323 — k_off = - s-1 -
CHEMBL5966583 — kon = - — -
CHEMBL5966583 — k_off = - s-1 -
CHEMBL5790628 — kon = - — -
CHEMBL5954468 — k_off = - s-1 -