BI-639667

BI 639667: Antagonist of CCR1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 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-639667 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CCR1

Antagonist

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P32246

Target Class: GPCR

Target SubClass: Chemokine Receptor

Potency: IC50

Potency Value: 5.4 nM

Potency Assay: CCR1 binding affinity Scintillation Proximity Assay binding

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

Target aliases:

, C-C chemokine receptor type 1, SCYAR1, CMKR1, CM ...

DOI Reference: 10.1016/j.bmcl.2018.12.024

Uniprot ID: P32246

Target Class: GPCR

Target SubClass: Chemokine Receptor

Potency: IC50

Potency Value: 24 nM

Potency Assay: CCR1 molecular potency, IC50= 24nM (Ca2+ flux)

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

Target aliases:

, C-C chemokine receptor type 1, SCYAR1, CMKR1, CM ...

DOI Reference: 10.1016/j.bmcl.2018.12.024

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Selectivity over other measured CCRs >1,000-fold. In Cerep panel of CCRs (>90% CTL for: CCR10, CCR9, CCR6, CCR4 @ 10 µm). Clean GPCR scan except for weak activity on ADRB1 (Ki = 1883.65 nM). Eurofins-Panlabs screen at 10 µM: ADORA2A: 69 % inhibition (not reproduced in dose response). Selectivity outside target family: Eurofins-Panlabs receptor screen on 69 targets @ 10 µM: 67 targets < 45 % inhibition, DATRANS 71 % inhibition (not reproduced in dose response)

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 15 Feb 2022 )