ChEMBL ligand: CHEMBL4576388
NTS1 receptor/Neurotensin receptor type 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
NTS1 receptor/Neurotensin receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
ChEMBL	NTR1 Ca2+ Flux Dose Response: 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 concentration of 1.0×106 cells per mL into black, 384-well assay plates with clear bottoms using a Multidrop liquid handler. Assay plates are incubated at 37° C. in 5% CO2. The next day, the assay plates are aspirated to remove growth media and washed once with 20 uL of DPBS. The DPBS is then aspirated from the assay plate and replaced with 25 uL of Fluo-4 NW calcium dye prepared according to the manufacturer's recommendations then the plates are incubated for 1 hour at 37° C. Following the incubation in the presence of dye, the assay is run on a Molecular Devices FlexStation-III using 494 excitation and 516 emission wavelengths set to read for 90 seconds with the addition at 18 seconds of 5 uL of 6× final concentration of test compounds and peptide control diluted in assay media containing 0.1% BSA and no more than 9% DMSO to yield a maximum final DMSO concentration of 1.5%. Percent activation is calculated based on the maximum response minus the minimum value over the time course relative to the neurotensin 1 control peptide at 100 pM. EC50 values were calculated for those compounds tested in 8-point dose dependent response.	B	6.3	pEC50	<500	nM	EC50	US-10118902-B2. Small molecule agonists of neurotensin receptor 1 (2018)
ChEMBL	NTR1 Ca2+ Flux Dose Response: 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 at a concentration of 1.0×106 cells per mL into black, 384-well assay plates with clear bottoms using a Multidrop liquid handler. Assay plates are incubated at 37° C. in 5% CO2. The next day, the assay plates are aspirated to remove growth media and washed once with 20 μL of DPBS. The DPBS is then aspirated from the assay plate and replaced with 25 μL of Fluo-4 NW calcium dye prepared according to the manufacturer's recommendations then the plates are incubated for 1 hour at 37° C. Following the incubation in the presence of dye, the assay is run on a Molecular Devices FlexStation-III using 494 excitation and 516 emission wavelengths set to read for 90 seconds with the addition at 18 seconds of 5 μL of 6× final concentration of test compounds and peptide control diluted in assay media containing 0.1% BSA and no more than 9% DMSO to yield a maximum final DMSO concentration of 1.5%. Percent activation is calculated based on the maximum response minus the minimum value over the time course relative to the neurotensin 1 control peptide at 100 μM. EC50 values were calculated for those compounds tested in 8-point dose dependent response.	B	6.3	pEC50	<500	nM	EC50	US-10584103-B2. Small molecule agonists of neurotensin receptor 1 (2020)
ChEMBL	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 beta-arrestin recruitment measured after 90 mins by pathhunter assay	B	6.47	pEC50	340	nM	EC50	J Med Chem (2019) 62: 8357-8363 [PMID:31390201]
ChEMBL	Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after 45 mins	B	6.85	pEC50	140	nM	EC50	J Med Chem (2019) 62: 8357-8363 [PMID:31390201]
ChEMBL	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-mediated calcium flux by measuring neurotensin EC50 at 0.0088 to 2.15 uM (Rvb = 0.035 nM)	F	8.93	pEC50	1.18	nM	EC50	J Med Chem (2019) 62: 8357-8363 [PMID:31390201]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]