Compound name
LDN-212854
Protein family
Protein Kinase
Target name
BMPR1A
Affinity biochemical (nM)
85.5
Affinity on-target cellular (nM)
166
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002066a
SMILES
N1(C2=CC=C(C(C=N3)=CN4C3=C(C5=C(C=CC=N6)C6=CC=C5)C=N4)C=C2)CCNCC1
InChIKey
BBDGBGOVJPEFBT-UHFFFAOYSA-N
NCBI gene ID
657
UniProt ID
P36894
Synonyms
ALK3, CD292
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay (using 6 µM ATP)
Affinity Biochemical Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Luciferase Reporter Assay (BRE-Luc, using C2C12 myofibroblast cells, caALK3)
Affinity on-target cellular source knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Nanosyn)
Selectivity platform number of targets
198
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: ABL1(95.7%), PDGFRB (94.1%), SIK2 (88%), ALB2(89%), MAP4K4 (84.4%), MINK (79.8%), full screening data available as supporting information; Screened at 100 nM, against 451 kinases (KinomeScan, DiscoverX), closest targets as % of control: ACVR1(100%), BMPR1A (98.8%), ABL1(phosphorylated, 97.8%), ABL1(H396P, phosphorylated, 97.5%), , ABL1(H396P, non-phosphorylated, 97.4%), KIT(V559D, 97.5%), PDGFRB (97.2%), ABL1(nonphosphorylated, 97.1%), ABL1(Q252H)-phosphorylated (96.9%), BMPR1B (96.5%), ABL1(Y253F)-phosphorylated (96.4%), KIT(95.8%), full screening data available as supporting information, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/;
Selectivity Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/
Selectivity Number of Off-targets
2