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Assay Detail

CHEMBL5729860

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

Binding
In Vitro Assay: The inhibitory activity of the compounds of this invention against the SGLT-1 or SGLT-2 transporters.
ChEMBL ↗
66
Total Activities
22
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium/glucose cotransporter 2 (CHEMBL3884) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SGLT-2 inhibitors, methods of making them, and uses thereof
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.82 7.94
kon 22 - -
k_off 22 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3660003 — — 3 7.94
CHEMBL3639588 — — 3 7.63
CHEMBL3288752 — — 3 7.44
CHEMBL3288738 — — 3 7.09
CHEMBL3288737 — — 3 7.08
CHEMBL3288744 — — 3 7.04
CHEMBL3288739 — — 3 7.02
CHEMBL3288745 — — 3 6.96
CHEMBL3288740 — — 3 6.89
CHEMBL3288741 — — 3 6.84
CHEMBL3660004 — — 3 6.83
CHEMBL3659998 — — 3 6.77
CHEMBL3288742 — — 3 6.65
CHEMBL3659997 — — 3 6.65
CHEMBL3660000 — — 3 6.65
CHEMBL3288746 — — 3 6.56
CHEMBL3659996 — — 3 6.50
CHEMBL3660002 — — 3 6.48
CHEMBL3659999 — — 3 6.33
CHEMBL3660005 — — 3 6.31
CHEMBL3660001 — — 3 6.27
CHEMBL3288743 — — 3 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3660003 — IC50 = 11.4 nM 7.94
CHEMBL3639588 — IC50 = 23.6 nM 7.63
CHEMBL3288752 — IC50 = 36.6 nM 7.44
CHEMBL3288738 — IC50 = 81.1 nM 7.09
CHEMBL3288737 — IC50 = 82.8 nM 7.08
CHEMBL3288744 — IC50 = 91.0 nM 7.04
CHEMBL3288739 — IC50 = 94.8 nM 7.02
CHEMBL3288745 — IC50 = 109.0 nM 6.96
CHEMBL3288740 — IC50 = 129.0 nM 6.89
CHEMBL3288741 — IC50 = 145.0 nM 6.84
CHEMBL3660004 — IC50 = 148.0 nM 6.83
CHEMBL3659998 — IC50 = 170.0 nM 6.77
CHEMBL3659997 — IC50 = 223.0 nM 6.65
CHEMBL3288742 — IC50 = 222.0 nM 6.65
CHEMBL3660000 — IC50 = 226.0 nM 6.65
CHEMBL3288746 — IC50 = 273.0 nM 6.56
CHEMBL3659996 — IC50 = 316.0 nM 6.50
CHEMBL3660002 — IC50 = 329.0 nM 6.48
CHEMBL3659999 — IC50 = 463.0 nM 6.33
CHEMBL3660005 — IC50 = 489.0 nM 6.31
CHEMBL3660001 — IC50 = 542.0 nM 6.27
CHEMBL3288743 — IC50 = 991.0 nM 6.00
CHEMBL3660003 — kon = - — -
CHEMBL3660004 — k_off = - s-1 -
CHEMBL3660003 — k_off = - s-1 -
CHEMBL3660004 — kon = - — -
CHEMBL3659996 — kon = - — -
CHEMBL3288737 — kon = - — -
CHEMBL3288737 — k_off = - s-1 -
CHEMBL3288740 — kon = - — -
CHEMBL3288740 — k_off = - s-1 -
CHEMBL3288746 — kon = - — -
CHEMBL3288746 — k_off = - s-1 -
CHEMBL3288744 — kon = - — -
CHEMBL3288744 — k_off = - s-1 -
CHEMBL3288743 — kon = - — -
CHEMBL3639588 — kon = - — -
CHEMBL3660002 — k_off = - s-1 -
CHEMBL3660002 — kon = - — -
CHEMBL3660001 — k_off = - s-1 -
CHEMBL3639588 — k_off = - s-1 -
CHEMBL3660001 — kon = - — -
CHEMBL3660000 — k_off = - s-1 -
CHEMBL3659998 — kon = - — -
CHEMBL3659998 — k_off = - s-1 -
CHEMBL3659999 — kon = - — -
CHEMBL3660005 — kon = - — -
CHEMBL3659999 — k_off = - s-1 -
CHEMBL3660005 — k_off = - s-1 -
CHEMBL3660000 — kon = - — -