BI-2081

BI-2081 : Agonist of FFAR1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe BI-2081 is in the process of SERP review.

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Information

FFAR1

Agonist

up to 200 nM
Reviewer recommended concentration: extracellular target

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: O14842

Target Class: GPCR

Target SubClass: Free fatty acid receptor

Potency: Ki

Potency Value: 23 nM

Potency Assay: Biochemical assay

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

Target aliases:

Free fatty acid receptor 1, GPR40, FFAR1, FFAR1_HU ...

Other Reference: Peer reviewed at SGC

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Eurofins Safety Panel (44 GPCRs at 10 μM): Closest off-targets (Kd [µM]): ADRA2C (0.840), ADRA2A (1.3), CHRM3 (2.9); HRH1 (3.1), PTGER4 (4.6), ADRA2B (21) Outside target family: Eurofins Safety Panel (29 receptor/channel targets at 10 μM): Closest off-targets (Kd [µM]): PPARG (0.470), THRA (rat, 3.5)

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SERP ratings and comments

SERP Ratings

In Model Organisms

(last updated: 19 Feb 2024 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

This is a well validated for in cell probe use. The in vivo data lack demonstration of target engagement, but PK properties reported and favorable.

(last updated: 14 Oct 2025 )