BDBM50072394 1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide::A-38579::ABBOTT-38579::PROTIRELIN

SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1

InChI Key InChIKey=XNSAINXGIQZQOO-SRVKXCTJSA-N

Data  7 KI  6 IC50  12 EC50

  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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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 50072394   

TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]N(1)-Me-His-TRH from TRHR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  10nMpH: 7.4Assay Description:Inhibitory constant against thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells upon incubation at 37 degee C for 1 hr at pH 7.4 us...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  10nMAssay Description:Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Homo sapiens (Human))
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]N(1)-Me-His-TRH from TRHR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  20nMpH: 7.4Assay Description:Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degee C for 1 hr at pH 7.4 us...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  23nMAssay Description:Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataKi:  42nMAssay Description:Inhibition of [3H]-[3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  23nMAssay Description:Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRHR2 expressed in HEK2935 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  2.30E+4nMAssay Description:Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRH2 receptor expressed in HEK2935 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3.20nMAssay Description:Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Mus musculus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  7nMAssay Description:Displacement of [3H]-Me-His-TRH from mouse TRH-R2 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  1nMAssay Description:Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Mus musculus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  0.5nMAssay Description:Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  26nMAssay Description:Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Mus musculus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3.10nMAssay Description:Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  0.490nMAssay Description:Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  0.680nMAssay Description:Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Mus musculus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  0.520nMAssay Description:Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  2.60nMAssay Description:Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Mus musculus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataIC50:  7nMAssay Description:Displacement of [3H]-1-MeHis-TRH from mouse TRH-R2 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3nMAssay Description:Agonist activity at TRHR2 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Homo sapiens (Human))
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3nMAssay Description:Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3nMpH: 7.8Assay Description:Signaling (activation) potency for thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(Rattus norvegicus)
National Institute Of Pharmaceutical Education And Research

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  3nMpH: 7.8Assay Description:Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThyrotropin-releasing hormone receptor(MOUSE)
Washington University

Curated by ChEMBL
LigandPNGBDBM50072394(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Affinity DataEC50:  1nMAssay Description:Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed