Compound name
TRULI
Protein family
Protein Kinase
Target name
LATS1
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
9113
UniProt ID
O95835
Synonyms
WARTS
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