BDBM50107283 AAT-007::CJ-023::Grapiprant::MR-10A7::RQ-00000007::RQ-7

SMILES CCc1nc2c(C)nc(C)cc2n1-c1ccc(CCNC(=O)NS(=O)(=O)c2ccc(C)cc2)cc1

InChI Key InChIKey=HZVLFTCYCLXTGV-UHFFFAOYSA-N

Data  11 KI  8 IC50

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 19 hits for monomerid = 50107283   

TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 12nMAssay Description:Antagonist activity at recombinant human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-stimulated cAMP accumulation by scinti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2016
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 689nMAssay Description:Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analy...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2016
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 1.61E+3nMAssay Description:Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha reduction preincubated for 3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2016
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 1.60E+3nMAssay Description:Antagonist activity at EP4 receptor in LPS-stimulated human whole blood assessed as inhibition of PGE2-induced TNF-alpha release pretreated for 30 mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/5/2017
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 1.52E+3nMAssay Description:Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/9/2017
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 12nMAssay Description:Antagonist activity against human EP4 expressed in HEK293 cells assessed as inhibition of PGE2-stimulated production of cAMP incubated for 20 mins by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/9/2017
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 1.52E+3nMAssay Description:Antagonist activity at EP4 receptor in human whole blood assessed as reversal of inhibition of PGE2 mediated LPS-induced TNF alpha production pretrea...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataIC50: 12nMAssay Description:Antagonist activity at human EP4 receptor in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi:  13nMAssay Description:Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi:  20nMAssay Description:Antagonist activity at rat recombinant EP4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi:  24nMAssay Description:Antagonist activity at dog recombinant EP4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi:  448nMAssay Description:Antagonist activity at human EP4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP4 subtype(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi:  449nMAssay Description:Displacement of [3H]-PGE2 from recombinant human EP4 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analy...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2016
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP3 subtype(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human EP3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetProstaglandin F2-alpha receptor(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human FP receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetProstacyclin receptor(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human IP receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP2 subtype(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human EP2 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetThromboxane A2 receptor(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human platelet TP receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed
TargetProstaglandin E2 receptor EP1 subtype(Human)
Askat

Curated by ChEMBL
LigandPNGBDBM50107283(AAT-007 | CJ-023 | Grapiprant | MR-10A7 | RQ-00000...)
Affinity DataKi: >5.00E+3nMAssay Description:Antagonist activity at human EP1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2019
Entry Details Article
PubMed