Compound name
BI-639667
Protein family
GPCR
Target name
CCR1
Affinity biochemical (nM)
5.4
Affinity on-target cellular (nM)
2.4
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000352a
SMILES
CS(C1=CC(C2(NC(C3=CN=CC4=C3C=NN4C5=CC=C(F)C=C5)=O)CC2)=CC=N1)(=O)=O
InChIKey
PXQATVYJKMMHAU-UHFFFAOYSA-N
NCBI gene ID
1230
UniProt ID
P32246
Synonyms
CKR-1, MIP1aR, CD191
Mode of action
Antagonist
Negative control
BI-9307
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation Proximity Assay (SPA)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI%20639667
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Chemotaxis in THP-1 cells
Affinity on-target cellular relation
=
Selectivity platform
GPCR panel (PDSP)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, closest target: Ki(ADRB1) = 1.88 µM; Screened in CEREP panel of CCRs at 10 µM: >1000-fold selective over other CCRs (CCR10, CCR9, CCR6, CCR4, all >90% of control); Screened against 69 receptors (Eurofins-Panlabs screen) at 10 µM, closest target as % inhibition: DATRANS (71%); Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: NRD2 (34%), LRRK2 (43%)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI%20639667
Selectivity Number of Off-targets
0