Compound name
RP-6306
Protein family
Protein Kinase
Target name
PKMYT1
Affinity biochemical (nM)
3.1
Affinity on-target cellular (nM)
14, 58, 138, 378, 262, 276, 4.8
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002949a
SMILES
O=C(C1=C(N)[N@]([C@]2=C(C)C(O)=CC=C2C)C3=NC(C)=C(C)C=C31)N
InChIKey
ARBRHWRTXPWZGN-UHFFFAOYSA-N
NCBI gene ID
9088
UniProt ID
Q99640
Synonyms
MYT1, PPP1R126
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
ADP-Glo assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/35444283/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
AlphaLISA (PKMYT1 dependent phoshorylation of CDK1 at Thr14 using FUOV1 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/35880755/
Affinity on-target cellular relation
=
Selectivity platform
Kinativ Colo-205 cell lysate kinase binding assay
Selectivity platform number of targets
274
Selectivity remarks
Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/35880755/
Selectivity Number of Off-targets
0