BDBM85050 CAS_184162-64-9::SR 142948A::SR142948::SR142948A::US20240287046, Compound C-3

SMILES CC(C)c1cc(ccc1n2c(cc(n2)C(=O)NC3(C4CC5CC(C4)CC3C5)C(=O)O)c6c(cccc6OC)OC)C(=O)N(C)CCCN(C)C

InChI Key InChIKey=LWULHXVBLMWCHO-UHFFFAOYSA-N

Data  9 KI  4 IC50  1 Kd  3 EC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 17 hits for monomerid = 85050   

TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataIC50: 2.35nMAssay Description:The binding affinities of test compounds were determined by a radioligand competitive binding assay using 177Lu labeled C-1 as the reference radiolig...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/12/2024
Entry Details
Go to US Patent

LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKd:  0.400nMAssay Description:The rat NTSR1 variant NTSR1-H4 was first expressed in E. coli using a derivative of the vector pRG/III-hsMBP. This construct had a C-terminally fused...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataEC50:  20nMAssay Description:Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataIC50: 4nMAssay Description:Antagonist activity at NTR1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataIC50: 3.20nMAssay Description:Displacement of [3H]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2017
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataIC50: 4nMAssay Description:Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2016
Entry Details Article
PubMed
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataEC50:  22nMAssay Description:Agonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2016
Entry Details Article
PubMed
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataEC50:  18nMAssay Description:Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/18/2016
Entry Details Article
PubMed
TargetNeurotensin(Guinea pig)
Sanofi Recherche

Curated by PDSP Ki Database
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  0.170nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2012
Entry Details
PubMed
TargetNeurotensin/neuromedin N(Human)
Sanofi Recherche

Curated by PDSP Ki Database
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  0.280nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2012
Entry Details
PubMed
TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  1nMAssay Description:Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Human)
Full-Life Technologies HK

US Patent
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [3H]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2017
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  1.40nMAssay Description:Displacement of [125I]neurotensin from rat NTS1 receptor expressed in CHO-K1 cells by competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2016
Entry Details Article
PubMed
TargetNeurotensin receptor type 1(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  2nMAssay Description:Displacement of [125L]NT from rat neurotensin receptor type 1 expressed in CHOK1 cells by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/18/2016
Entry Details Article
PubMed
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  5.80nMAssay Description:Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2016
Entry Details Article
PubMed
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  6nMAssay Description:Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMed
TargetNeurotensin receptor type 2(Rat)
Research Triangle Institute

Curated by ChEMBL
LigandPNGBDBM85050(SR142948A | CAS_184162-64-9 | SR 142948A | SR14294...)
Affinity DataKi:  7nMAssay Description:Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/18/2016
Entry Details Article
PubMed