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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
