BDBM328993 5-[[4-[[(2R)-morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile::US11787792, Compound 1::US9663503, Compound 1

SMILES FC(F)(F)c1cnc(Nc2cnc(cn2)C#N)cc1NC[C@H]1CNCCO1

InChI Key InChIKey=YBYYWUUUGCNAHQ-UHFFFAOYSA-N

Data  23 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 45 hits for monomerid = 328993   

TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of CHK1 (unknown origin) using 5-FAM-KKKVSRSGLYRSPSMPENLNRPR-COOH peptide as substrate incubated for 1 hr in presence of ATP by caliper mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.40nMAssay Description:CHK1 kinase activity was measured in a microfluidic assay that monitors the separation of a phosphorylated product from its substrate. The assay was ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/4/2019
Entry Details
US Patent

TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.40nMAssay Description:CHK1 kinase activity was measured in a microfluidic assay that monitors the separation of a phosphorylated product from its substrate. The assay was ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/29/2023
Entry Details
US Patent

TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of recombinant human CHK1 by microfluidic assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 2nMAssay Description:Inhibition of CHK1 (unknown origin) using Cdc25 peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 4.30nMAssay Description:Inhibition of CHK1 (unknown origin) preincubated with compound for 10 mins followed by ATP addition and measured after 50 mins by fluorescence based ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 26nMAssay Description:Inhibition of CHK1 (unknown origin) using peptide substrate incubated for 1 hrs in presence of ATP by fluorescence microplate reader analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 29nMAssay Description:Inhibition of CHK1 (unknown origin) using peptide substrate S1 and ATP as substrate incubated for 1 hr by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 30nMAssay Description:Inhibition of CHK1 in human HT-29 cells assessed as abrogation of etoposide-induced G2 checkpoint arrest by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 30nMAssay Description:Inhibition of CHK1 in etoposide-induced human HT-29 cells assessed as G2 checkpoint abrogation in presence of nocodazole by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 63nMAssay Description:Inhibition of CHK1 in etoposide-induced human MIA PaCa-2 cells assessed as G2 checkpoint abrogation in presence of nocodazole by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 84nMAssay Description:Inhibition of CHK1 in etoposide-induced human Calu-6 cells assessed as G2 checkpoint abrogation in presence of nocodazole by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetMitogen-activated protein kinase 15(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 130nMAssay Description:Inhibition of human ERK8 in presence of ATP by by radiometric kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk1(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 220nMAssay Description:Inhibition of CHK1 in etoposide-induced human SW620 cells assessed as G2 checkpoint abrogation in presence of nocodazole by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase D1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 298nMAssay Description:Inhibition of PRKD1 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetRibosomal protein S6 kinase alpha-3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 361nMAssay Description:Inhibition of human RSK2 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetRibosomal protein S6 kinase alpha-1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 362nMAssay Description:Inhibition of human RSK1 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 582nMAssay Description:Inhibition of FLT3 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetMAP/microtubule affinity-regulating kinase 3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 698nMAssay Description:Inhibition of human MARK3 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetNUAK family SNF1-like kinase 1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 711nMAssay Description:Inhibition of human NUAK1 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 910nMAssay Description:Inhibition of wildtype FLT3 (unknown origin) using peptide substrate incubated for 1 hrs in presence of ATP by fluorescence microplate reader analysi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk2(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.26E+3nMAssay Description:Inhibition of human CHK2 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetDual specificity protein kinase CLK2(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.37E+3nMAssay Description:Inhibition of human CLK2 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase BRSK1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.66E+3nMAssay Description:Inhibition of human BRSK1 by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.97E+3nMAssay Description:Inhibition of FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for 1 hrs in presence of ATP by fluorescence microplate reader ana...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 2.10E+3nMAssay Description:Inhibition of VEGFR2 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk2(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 2.44E+3nMAssay Description:Inhibition of human CHK2 by microfluidic assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 2.97E+3nMAssay Description:Inhibition of AMPK alpha1/beta1/gamma1 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPhosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 3.47E+3nMAssay Description:Inhibition of PHKG1 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 6.20E+3nMAssay Description:Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 9.03E+3nMAssay Description:Inhibition of CDK1/CyclB (unknown origin) in presence of ATP by DELFIA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human HCN4More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human KCNQ1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human Kv4.3More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetInward rectifier potassium channel 2(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human Kir2.1More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human L-type calcium channel Cav1.2More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human Nav1.5More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human Kv1.5More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 2C19(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCytochrome P450 2A6(Human)
Sareum

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of CYP2A6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetVascular endothelial growth factor receptor 1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM328993(US9663503, Compound 1 | 5-[[4-[[(2R)-morpholin-2-y...)
Affinity DataIC50: 1.58E+4nMAssay Description:Inhibition of VEGFR1 (unknown origin) by FRET based Z-LYTE kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed