Compound name
TRULI
Protein family
Protein Kinase
Target name
LATS2
Affinity biochemical (nM)
0.2
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001910a
SMILES
O=C(C1=CNC2=NC=CC=C12)/N=C(SC=C3)/N3CC4=CC=CC=C4
InChIKey
VTXBMVZVPUSAJF-UZYVYHOESA-N
NCBI gene ID
26524
UniProt ID
Q9NRM7
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay (using 10 µM ATP)
Affinity Biochemical Source Knowledge
https://www.nature.com/articles/s41467-021-23395-3#Sec31
Affinity biochemical relation
=
Selectivity platform
Kinase panel (literature)
Selectivity platform number of targets
314
Selectivity remarks
Screened at 1 µM, closest targets as % affinity: CLK4 (102.2%), PRKCQ (99.2%), CDC7 (99.1%), DMPK (97.9%), CDC42BPA (97.2%), HIPK3 (95.8%), HIPK2 (94.2%), PRKACB (92.9%), CLK2 (92.8%), GSK3B (92.7%), PRKCH (90.4%), CDK19 (90.2%), LATS1 (73.9%), LATS2 (74.9%), further screening data are available as supporting info, https://static-content.springer.com/esm/art%3A10.1038%2Fs41467-021-23395-3/MediaObjects/41467_2021_23395_MOESM1_ESM.pdf;
In-vitro potency (HTFR assay): IC50(PRKA) = 60 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(PRKCE) = 14 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(ROCK1) = 88 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(NDR1) = 1000 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(PRKA) = 60 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(PRKCE) = 14 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(ROCK1) = 88 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
In-vitro potency (HTFR assay): IC50(NDR1) = 1000 nM, https://www.nature.com/articles/s41467-021-23395-3#Sec11;
Selectivity Source Knowledge
https://www.nature.com/articles/s41467-021-23395-3#Sec11
Selectivity Number of Off-targets
12