neurokinin A [Ligand Id: 2089] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL217406 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 6.2 | pKi | 630 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1369-1374 [PMID:9871768] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
Br J Pharmacol (2002) 135: 266-74 [PMID:11786503]; FEBS Lett (1996) 399: 264-266 [PMID:8985159]; FEBS Lett (1992) 296: 241-4 [PMID:1311270]; J Pharmacol Exp Ther (1997) 281: 1303-11 [PMID:9190866] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Tested for inhibition of tachykinin 1 (NK1) receptor in rat brain synaptosomal membranes using [125I]BH-SP as radioligand | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 447-450 |
| ChEMBL | Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 559-564 |
| Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547] | ||||||||
| ChEMBL | Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral cortex membranes was determined using [3H]SP as the radioligand | B | 8.46 | pIC50 | 3.5 | 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 | 7.86 | pEC50 | 13.7 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | Binding affinity against F293A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 7.4 | pKd | 40 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against F112A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 7.97 | pKd | 10.7 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Q166A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.18 | pKd | 6.6 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Y206F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.23 | pKd | 5.9 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against T171A human neurokinin-2 receptor (hNK-2R) using [125I]-NKA as a radioligand | B | 8.23 | pKd | 5.9 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Y269F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.28 | pKd | 5.3 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Q109A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.49 | pKd | 3.2 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Y266F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.55 | pKd | 2.8 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against S164A human neurokinin-2 receptor (hNK-2R) using [125I]-NKA as a radioligand | B | 8.6 | pKd | 2.5 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against wild type human Wild-type tachykinin receptor 2 (hNK-2R) using [125I]NKA as a radioligand | B | 8.62 | pKd | 2.4 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against F168A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.64 | pKd | 2.3 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against I202F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.68 | pKd | 2.1 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Y289F human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.7 | pKd | 2 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against S170A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 8.72 | pKd | 1.9 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Binding affinity against Y107A human neurokinin-2 receptor (hNK-2R) using [125I]NKA as a radioligand | B | 9.3 | pKd | 0.5 | nM | KD/Ki | J Med Chem (2002) 45: 3418-3429 [PMID:12139452] |
| ChEMBL | Displacement of [3H]GR100679 from NK2 receptor (unknown origin) expressed in CHO/T cells | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2014) 57: 8187-8203 [PMID:24983484] |
| GtoPdb | - | - | 9.1 | 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]; Biochem Pharmacol (2001) 61: 55-60 [PMID:11137709] |
| ChEMBL | The compound was tested for competition binding with [3H]NKA against the CHO cells from cloned human Tachykinin receptor 2 | B | 9.15 | pKi | 0.71 | nM | Ki | J Med Chem (1999) 42: 3004-3007 [PMID:10425111] |
| ChEMBL | Tested for the binding affinity to human NK2 receptor expressed in Sf-9 insect larval cells using 0.1 nM 2-[125 I] iodohistidyl neurokinin A | F | 8.11 | pIC50 | 7.7 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 715-718 |
| ChEMBL | Inhibitory activity against human Tachykinin receptor 2 | B | 8.77 | pIC50 | 1.7 | 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 | 9 | pIC50 | 1 | 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 | Allosteric modulation of rat NK2 receptor expressed in HEK293 cells assessed as cAMP production by radioimmunoassay | F | 7.19 | pEC50 | 64.8 | nM | EC50 | J Med Chem (2009) 52: 5999-6011 [PMID:19746979] |
| ChEMBL | In vitro agonistic activity against tachykinin receptor 2 of rat colon muscularis mucosae. | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
| ChEMBL | Allosteric modulation of rat NK2 receptor expressed in HEK293 cells assessed as increase in intracellular calcium level by spectrofluorimetry | F | 9.26 | pEC50 | 0.55 | nM | EC50 | J Med Chem (2009) 52: 5999-6011 [PMID:19746979] |
| Neurokinin 2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2647] [UniProtKB: Q64077] | ||||||||
| ChEMBL | Evaluated for the binding affinity against NK2 receptor | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (1993) 36: 3197-3201 [PMID:7693945] |
| NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371] | ||||||||
| GtoPdb | - | - | 6.3 | 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 | 7.35 | pIC50 | 45 | 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 | 7.28 | pEC50 | 53 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1343-1348 [PMID:9871763] |
| GtoPdb | - | - | 7.4 | pEC50 | 40 | nM | EC50 | FEBS Lett (1992) 299: 90-5 [PMID:1312036] |
| NK3 receptor in Mouse [GtoPdb: 362] [UniProtKB: P47937] | ||||||||
| GtoPdb | - | - | 6.1 | 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 | In vitro agonistic activity against tachykinin receptor 3 of everted rat protal vein. | F | 6.25 | pEC50 | 563 | nM | EC50 | J Med Chem (1992) 35: 4195-4204 [PMID:1331460] |
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]
