Compile Data Set for Download or QSAR
Report error Found 6 Enz. Inhib. hit(s) for PDB: 8JPB
LigandPNGBDBM130909(US8822500, Stauro- sporine | US9920060, Staurospor...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human GRK2 using casein as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details PDB3D3D Structure (crystal)
TargetNeurotensin receptor type 1(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM297513(US10118902, Example 15 | 2-({2-(1-Fluoro-cycloprop...)
Affinity DataEC50:  1.20nMAssay Description:Positive allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as effect on NT (8 to 13) peptide-media...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeurotensin receptor type 1(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM297513(US10118902, Example 15 | 2-({2-(1-Fluoro-cycloprop...)
Affinity DataEC50:  140nMAssay Description:Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeurotensin receptor type 1(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM297513(US10118902, Example 15 | 2-({2-(1-Fluoro-cycloprop...)
Affinity DataEC50:  340nMAssay Description:Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated be...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeurotensin receptor type 1(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM297513(US10118902, Example 15 | 2-({2-(1-Fluoro-cycloprop...)
Affinity DataEC50: <500nMAssay Description:NTSR1 (NTR1) CHO cells are plated in 20 μL of assay media containing Ham's F12 supplemented with 10% fetal bovine serum and 0.4 mg/mL G418 a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/29/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetNeurotensin receptor type 1(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandPNGBDBM297513(US10118902, Example 15 | 2-({2-(1-Fluoro-cycloprop...)
Affinity DataEC50: <500nMAssay Description:NTSR1 (NTR1) CHO cells are plated in 20 uL of assay media containing Ham's F12 supplemented with 10% fetal bovine serum and 0.4 mg/mL G418 at a c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/11/2019
Entry Details
US Patent
PDB3D3D Structure (crystal)