BAY-876

Inhibitor of SLC2A1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe BAY-876 is in the process of SERP review.

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Information

SLC2A1

Inhibitor

up to 100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P11166

Target Class: Transporter

Target SubClass: Solute Carrier

Potency: IC50

Potency Value: 2 nM

Potency Assay: Inhibition of glucose uptake measured by measuring ATP levels using CellTiter-Glo Luminescent Cell viability assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Solute carrier family 2, facilitated glucose trans ...

DOI Reference: 10.1002/cmdc.201600276

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: the closest target is SLC2A4 which is >100x less selective (IC50 = 270 nM); IC50 SLC2A2 = 9.4 µM; IC50 SLC2A3 = 1.6 µM. Selectivity outside target family: Closest off-targets: ADORA3 (IC50 = 1.14 µM); PTGER4 (IC50 = 1.12 µM) (Eurofins panel #68, others > 5 µM); clean for 18 tested kinases (all > 20 µM) ; Clean GPCR scan with the closest hit on HTR2 (pKi = 5.1)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 29 Nov 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 3 Dec 2021 )