BDBM6760 (+)-K-252a::CHEMBL281948::K-252a::US20250129067, Compound K252a::methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaene-16-carboxylate

SMILES COC(=O)[C@@]1(O)C[C@H]2O[C@]1(C)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13

InChI Key InChIKey=KOZFSFOOLUUIGY-UHFFFAOYSA-N

Data  1 KI  26 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 27 hits for monomerid = 6760   

LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 250nMAssay Description:Inhibition of protein kinase C (PKC)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha(Human)
Progentos Therapeutics

US Patent
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 427nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/25/2025
Entry Details
Go to US Patent

TargetSerine/threonine-protein kinase D1(Human)
University of Pittsburgh

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 7nMAssay Description:Inhibition of PKD1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetRho-associated protein kinase 2(Human)
Zhejiang University

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 500nMAssay Description:Inhibition of N-terminal His10-StrepII tagged human ROCK2 catalytic domain (1 to 553 residues) expressed in Sf9 insect cells by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 25nMAssay Description:Inhibition of TRKA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetMitogen-activated protein kinase kinase kinase 11(Human)
Chungnam National University

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 5nMAssay Description:Inhibition of N-terminal HA-tagged recombinant wild-type human MLK3 overexpressed in HEK293A cells preincubated for 10 mins followed by [gamma-32P]AT...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
TargetMitogen-activated protein kinase kinase kinase 11(Human)
Chungnam National University

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 5nMAssay Description:Inhibition of recombinant human N-terminal HA-tagged wild type MLK3More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
TargetProtein kinase C theta type(Human)
Zhejiang University

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 530nMAssay Description:Inhibition of PKCtheta (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetProtein kinase C zeta type(Rat)
Cephalon

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 250nMAssay Description:Inhibition of protein kinase CMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
TargetProtein kinase C zeta type(Rat)
Cephalon

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 60nMAssay Description:In vitro inhibition of protein kinase C from rat brain.More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2020
Entry Details Article

LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 60nMAssay Description:Inhibition of protein kinase C (PKC) isozymeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2020
Entry Details Article

LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 33nMAssay Description:Inhibition of protein kinase CMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2018
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 13nMAssay Description:Inhibition of baculovirus expressed human trkAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 25nMAssay Description:Inhibition of protein kinase CMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2018
Entry Details

LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 30nMpH: 7.0 T: 2°CAssay Description:In vitro CDK assay using purified enzyme, was incubated at room temperature with substrate, and test compounds in the presence of ATP/[gamma-33P]ATP....More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2005
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase(Rabbit)
Kyowa Hakko Kogyo

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 0.0160nMAssay Description:Inhibition of cAMP dependent Protein kinase A of rabbit Skeletal Muscle.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 2.40nMAssay Description:Ability to inhibit human trk A tyrosine kinase expressed in baculovirus using ELISA based enzyme assay was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetMyosin light chain kinase, smooth muscle(Chicken)
Kyowa Hakko Kogyo

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 0.0200nMAssay Description:Inhibition of Smooth muscle myosin light chain kinase of chicken gizzardMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetMyosin light chain kinase, smooth muscle(Human)
Cephalon

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 22nMAssay Description:Inhibition of Myosin light chain kinase 1 (MLCK1)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 13nMAssay Description:Inhibition of nerve growth factor receptor, trkAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 43nMAssay Description:Inhibition of VEGF-receptor 2 (KDR)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase pim-1(Human)
Vertex Pharmaceuticals

LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 150nMpH: 7.6 T: 2°CAssay Description:A coupled-enzyme assay was used to quantify the ADP generated in the kinase reaction with S6 peptide (RRRLSSLRA) as the phosphoacceptorsubstrate.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/3/2007
Entry Details Article
PubMed
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 45nMAssay Description:The MLK1, MLK2, and MLK3 assays were performed using the Millipore multiscreen trichloroacetic acid (TCA) in-plate format. IC50 values were calculate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2007
Entry Details Article
PubMed
TargetMitogen-activated protein kinase kinase kinase 11(Human)
Chungnam National University

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 13nMAssay Description:The MLK1, MLK2, and MLK3 assays were performed using the Millipore multiscreen trichloroacetic acid (TCA) in-plate format. IC50 values were calculate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2007
Entry Details Article
PubMed
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 22nMpH: 7.2 T: 2°CAssay Description:The MLK1, MLK2, and MLK3 assays were performed using the Millipore multiscreen trichloroacetic acid (TCA) in-plate format. IC50 values were calculate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2007
Entry Details Article
PubMed
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataIC50: 260nMT: 2°CAssay Description:In vitro CDK assay using purified enzyme, was incubated at room temperature with substrate, and test compounds in the presence of ATP/[gamma-33P]ATP....More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2005
Entry Details Article
PubMed
TargetMyosin light chain kinase, smooth muscle(Human)
Cephalon

Curated by ChEMBL
LigandPNGBDBM6760(CHEMBL281948 | methyl (15S,16R,18R)-16-hydroxy-15-...)
Affinity DataKi:  20nMAssay Description:Inhibition of MLCK by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2011
Entry Details Article
PubMed