Compound name
TP_030_2
Protein family
Protein Kinase
Target name
RIPK1
Affinity biochemical (nM)
0.43
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000720a
SMILES
CN1C([C@@H](N2CCC3=C(Br)N(CC4=CC=CC=C4)N=C3C2=O)COC5=C1C=CC=C5)=O
InChIKey
KHVVJKLNKLQLJZ-SFHVURJKSA-N
NCBI gene ID
8737
UniProt ID
Q13546
Synonyms
RIP
Mode of action
Allosteric inhibitor
Negative control
TP_030_n
Affinity biochemical definition
Ki
Affinity biochemical assay type
TR-FRET binding assay (Invitrogen)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-030-2
https://doi.org/10.1021/acs.jmedchem.7b01647
Affinity biochemical relation
=
Selectivity platform
Takeda global kinase panel
Selectivity platform number of targets
303
Selectivity remarks
Highly selective; Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(GABA/PBR) = 346.58 nM, Ki(HTR2A) = 2071.02 nM, Ki(ADRA2A) = 2355.74 nM; Screened in Eurofins-Panlabs radioligand binding assay against 68 targets at 10 µM: closest target: HTR2B (63 % of contr.)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-030-2
Selectivity Number of Off-targets
0