substance P [Ligand Id: 2098] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL235363 (Neurokinin p, Neuropeptide sp-1, Sh-oligopeptide-73, Substance p, Substance p (1-11)) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847] | ||||||||
| ChEMBL | Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay | F | 7.18 | pEC50 | 66 | nM | EC50 | J Med Chem (2020) 63: 10796-10815 [PMID:32882134] |
| NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
| ChEMBL | Compound was evaluated for affinity towards human tachykinin NK-1 receptor expressed in CHO cells | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1369-1374 [PMID:9871768] |
| GtoPdb | - | - | 10.3 | pKi | - | - | - |
Br J Pharmacol (2002) 135: 266-74 [PMID:11786503]; Bioorg Med Chem (2004) 12: 4533-41 [PMID:15265501] |
| ChEMBL | Tested for binding affinity against Q165A mutant NK1 receptor expressed in CHO cells, using [125]SP as radioligand | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2000) 43: 3827-3831 [PMID:11052787] |
| ChEMBL | Displacement of [125I]BH-SP to human recombinant NK1 receptor in CHO cells | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2008) 16: 6850-6859 [PMID:18554914] |
| ChEMBL | Displacement of [125I]BH-SP from human recombinant NK1 receptor expressed in CHO cells after 90 mins | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2011) 19: 2242-2251 [PMID:21421318] |
| ChEMBL | Tested for binding affinity against human wild type NK1 receptor expressed in CHO cells, using [125]SP as radioligand. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2000) 43: 3827-3831 [PMID:11052787] |
| ChEMBL | Tested for binding affinity against H265A mutant NK1 receptor using [125]SP radioligand in COS cells. | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2000) 43: 3827-3831 [PMID:11052787] |
| ChEMBL | Tested for binding affinity against H197A mutant NK1 receptor using [125]SP radioligand in COS cells. | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2000) 43: 3827-3831 [PMID:11052787] |
| ChEMBL | Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells | F | 9.21 | pIC50 | 0.61 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 281-284 [PMID:9871670] |
| ChEMBL | Inhibitory activity against binding of [125I]Bolton-Hunter SP to tachykinin NK-1 receptor in human lymphoma IM9 cells. | B | 9.59 | pIC50 | 0.26 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 165-166 |
| ChEMBL | Compound was evaluated for the antagonistic activity against NK1 receptor | F | 9.62 | pIC50 | 0.24 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2819-2824 |
| ChEMBL | Binding affinity against human Tachykinin receptor 1 expressed in astrocytoma UC11MG cells using [125I]- SP radioligand | B | 9.92 | pIC50 | 0.12 | nM | IC50 | J Med Chem (2004) 47: 1315-1318 [PMID:14998319] |
| ChEMBL | Agonist activity at bfSPR to produce increase in intracellular [Ca2+] | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2000) 43: 1741-1753 [PMID:10794691] |
| ChEMBL | SP-induced [Ca2+] mobilization in CHO cells expressing human Tachykinin receptor 1 | B | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2000) 43: 1741-1753 [PMID:10794691] |
| ChEMBL | Agonist activity at wild type human NK1 receptor expressed in HEK293 cells assessed as increase in [3H]IP accumulation after 20 mins | F | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2012) 55: 5061-5076 [PMID:22574973] |
| ChEMBL | Antagonist activity at human recombinant NK1 receptor expressed in CHO cells assessed as inhibition of NPS-induced intracellular calcium mobilization | F | 10.24 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2009) 52: 4068-4071 [PMID:19473027] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Ability to inhibit the binding of [125I]physalaemin to the SP receptors in rat telencephalon slices | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1987) 30: 1529-1532 [PMID:2441057] |
| ChEMBL | Affinity for rat Tachykinin receptor 1 determined in displacement screening by using radioligand 3,4-[3H]-(L-Pro e2) SP. | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (1999) 42: 4331-4342 [PMID:10543877] |
| ChEMBL | Displacement of [Leu-3,4,5-3H(N)]-Substance P from NK1 receptor in rat brain homogenate measured after 60 mins by microbeta scintillation counting analysis | B | 8.96 | pIC50 | 1.09 | nM | IC50 | ACS Med Chem Lett (2017) 8: 73-77 [PMID:28105278] |
| ChEMBL | Concentration required to inhibit the specific binding of [125I]BH-SP to Neurokinin-1 (NK-1) receptor in rat brain synaptosomes | B | 9.19 | pIC50 | 0.64 | nM | IC50 | J Med Chem (1994) 37: 1586-1601 [PMID:7515443] |
| ChEMBL | Displacement of [125I]Lys3-substance P from rat NK1 receptor expressed in CHO cells | B | 9.39 | pIC50 | 0.41 | nM | IC50 | J Med Chem (2007) 50: 6501-6506 [PMID:18067242] |
| ChEMBL | Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal membranes using [125I]BH-SP as radioligand | B | 9.43 | pIC50 | 0.37 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 447-450 |
| ChEMBL | Binding affinity for tachykinin receptor 1 from rat forebrain tissue, [125I]-BH-SP as radioligand | B | 9.92 | pIC50 | 0.12 | nM | IC50 | J Med Chem (1991) 34: 1751-1753 [PMID:1851847] |
| ChEMBL | Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand | B | 9.92 | pIC50 | 0.12 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 559-564 |
| ChEMBL | Inhibition of Tachykinin receptor 1 of rat forebrain tissue | B | 9.92 | pIC50 | 0.12 | nM | IC50 | J Med Chem (1992) 35: 1273-1279 [PMID:1373191] |
| ChEMBL | Inhibition of [125]I-Bolton Hunter Substance P([125]I-BHSP) binding to standard Tachykinin receptor 1 from rat forebrain membranes. | B | 9.92 | pIC50 | 0.12 | nM | IC50 | J Med Chem (1992) 35: 374-378 [PMID:1370695] |
| Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547] | ||||||||
| ChEMBL | Evaluated for the binding affinity against NK1 receptor | B | 7.3 | pKi | 50.5 | nM | Ki | J Med Chem (1993) 36: 3197-3201 [PMID:7693945] |
| ChEMBL | Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral cortex membranes was determined using [3H]SP as the radioligand | B | 10.15 | pIC50 | 0.07 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 559-564 |
| ChEMBL | In vitro agonistic activity against tachykinin receptor 1 of guinea pig ileum longitudinal smooth muscle. | F | 8.25 | pEC50 | 5.6 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| ChEMBL | Agonistic activity at neurokinin-1 (NK-1) receptor in guinea pig ileum longitudinal smooth muscle | F | 8.31 | pEC50 | 4.91 | nM | EC50 | J Med Chem (1990) 33: 1848-1851 [PMID:1694545] |
| ChEMBL | Agonistic activity at tachykinin receptor 1 receptor in guinea pig ileum longitudinal smooth muscle | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (1990) 33: 1848-1851 [PMID:1694545] |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
Br J Pharmacol (2002) 135: 266-74 [PMID:11786503]; J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]; Biochem Biophys Res Commun (1993) 191: 1172-7 [PMID:7682062] |
| ChEMBL | The compound was tested for competition binding with [3H]NKA against the CHO cells from cloned human Tachykinin receptor 2 | B | 6.99 | pKi | 102 | nM | Ki | J Med Chem (1999) 42: 3004-3007 [PMID:10425111] |
| ChEMBL | Inhibitory activity against human Tachykinin receptor 2 | B | 6.61 | pIC50 | 245.47 | nM | IC50 | J Med Chem (1999) 42: 3004-3007 [PMID:10425111] |
| Neurokinin 2 receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304405] [UniProtKB: P51144] | ||||||||
| ChEMBL | Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykinin receptor 2 | B | 6.83 | pIC50 | 148 | nM | IC50 | J Med Chem (1992) 35: 3949-3955 [PMID:1331450] |
| NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610] | ||||||||
| ChEMBL | Concentration required to inhibit the specific binding of [125I]NKA to Neurokinin-2 (NK-2) receptor in rat duodenum membranes | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1994) 37: 1586-1601 [PMID:7515443] |
| ChEMBL | Agonist activity was measured at neurokinin-2 receptor in the rat colon muscularis mucosae | F | 6.78 | pEC50 | 167.4 | nM | EC50 | J Med Chem (1990) 33: 1848-1851 [PMID:1694545] |
| ChEMBL | In vitro agonistic activity against tachykinin receptor 2 of rat colon muscularis mucosae. | F | 6.78 | pEC50 | 167 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| ChEMBL | Agonist activity at tachykinin receptor 2 in the rat colon muscularis mucosae | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (1990) 33: 1848-1851 [PMID:1694545] |
| NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866]; Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells | B | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| ChEMBL | Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells | F | 6.1 | pEC50 | 793 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - | Eur J Pharmacol (2001) 413: 143-50 [PMID:11226387] |
| NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177] | ||||||||
| ChEMBL | Concentration required to inhibit the specific binding of [125I]BH-ELE to Neurokinin-3 (NK-3) receptor in rat brain synaptosomes | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1994) 37: 1586-1601 [PMID:7515443] |
| ChEMBL | In vitro agonistic activity against tachykinin receptor 3 of everted rat protal vein. | F | 5.12 | pEC50 | 7500 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098] | ||||||||
| ChEMBL | Inhibitory activity against binding of [125I][MePhe7]-NKB SP to tachykinin NK-3 receptor in guinea pig cortical membranes. | B | 6.14 | pIC50 | 717 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 165-166 |
| MRGPRX2 in Human [GtoPdb: 157] [UniProtKB: Q96LB1] | ||||||||
| GtoPdb | In a calcium mobilisation asay. | - | 5.97 | pEC50 | 1071 | nM | EC50 |
Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]; Nature (2015) 519: 237-41 [PMID:25517090] |
ChEMBL data shown on this page come from version 34:
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]
