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 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]
