Compound name
LDN-193189
Protein family
Protein Kinase
Target name
BMPR1B
Affinity biochemical (nM)
16.7
Affinity on-target cellular (nM)
238
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002065aCl
SMILES
N1(C2=CC=C(C(C=N3)=CN4C3=C(C5=CC=NC6=C5C=CC=C6)C=N4)C=C2)CCNCC1.Cl.Cl
InChIKey
CDOVNWNANFFLFJ-UHFFFAOYSA-N
NCBI gene ID
658
UniProt ID
O00238
Synonyms
ALK6, CDw293
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay (using 6 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23646137/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Luciferase Reporter Assay (CAGA-Luc, using C2C12 myofibroblast cells, caALK4)
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
200
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: SIK1 (96%), ABL1(84%), MAP4K4(81%), PDGFRB(75%), full screening data available as supporting information; Data also available at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/; Screened at 100 nM, against 451 kinases (KinomeScan, DiscoverX), closest targets as % of control: ACVR1(99.9%), ACVR2A (95.8%), KIT(V559D, 95.4%), BMPR1B(95.3%), TGFBR2(93.8%), RIPK2(93.7%), BMPR1A(93%), ZAK(92%), ABL1(H396P, non-phosphorylated, 89%), full screening data available as supporting information, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901569/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23646137/
Selectivity Number of Off-targets
1