ChEMBL ligand: CHEMBL22870 (L-732138)
NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] NK1 receptor/Neurokinin 1 receptor in Rat [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] Neurokinin 2 receptor in Rabbit [ChEMBL: CHEMBL3433] [UniProtKB: P79218] NK2 receptor/Neurokinin 2 receptor in Rat [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610] There should be some charts here, you may need to enable JavaScript!
NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371] NK3 receptor/Neurokinin 3 receptor in Rat [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177] 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
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL	Antagonistic potency for NK-1 receptor was determined in vitro, using isolated rabbit vena cava.	F	8.4	pKd	3.98	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	6.87	pKi	134	nM	Ki	J Med Chem (2007) 50: 2779-2786 [PMID:17516639]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membranes	B	9.14	pKi	0.73	nM	Ki	Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL	Displacement of [3H]substance P frome human NK1 receptor	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2011) 54: 2029-2038 [PMID:21366266]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	6.4	pIC50	398.11	nM	IC50	J Med Chem (2007) 50: 2779-2786 [PMID:17516639]
ChEMBL	Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (1995) 38: 934-941 [PMID:7535362]
ChEMBL	Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	B	8.48	pIC50	3.3	nM	IC50	J Med Chem (1995) 38: 934-941 [PMID:7535362]
ChEMBL	Binding affinity was measured against the Tachykinin receptor 1 in CHO-expressed hNK1 using [125I]SP.	B	8.49	pIC50	3.24	nM	IC50	J Med Chem (1998) 41: 3609-3623 [PMID:9733486]
ChEMBL	Binding affinity at human Tachykinin receptor 1 expressed in CHO cells by [125 I]Trp8-substance P displacement.	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (1995) 38: 923-933 [PMID:7699709]
GtoPdb	Antagonism of [125]-substance P binding, to NK1 receptors expressed in CHO cells.	-	8.64	pIC50	2.3	nM	IC50	J Biol Chem (1994) 269: 6587-91 [PMID:7509807]
ChEMBL	Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (1995) 38: 934-941 [PMID:7535362]
ChEMBL	Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (1993) 36: 2044-2045 [PMID:8393115]
ChEMBL	Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined	B	8.8	pIC50	1.6	nM	IC50	Bioorg Med Chem Lett (1998) 8: 2259-2262 [PMID:9873524]
ChEMBL	Binding affinity towards cloned neurokinin 1 receptor, based on the displacement of [125I]-labeled substance P	B	8.8	pIC50	1.6	nM	IC50	J Med Chem (1994) 37: 1269-1274 [PMID:7513763]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting	B	8.8	pIC50	1.58	nM	IC50	J Med Chem (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	8.8	pIC50	-8.8	-	logIC50	J Med Chem (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane	B	8.83	pIC50	1.48	nM	IC50	J Med Chem (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membranes	B	8.83	pIC50	1.48	nM	IC50	Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL	Displacement of [3H]substance P frome human NK1 receptor	B	8.83	pIC50	1.48	nM	IC50	J Med Chem (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL	Displacement of [3H]substance P from human NK1 receptor expressed in CHO cells	B	8.83	pIC50	1.48	nM	IC50	J Med Chem (2011) 54: 2029-2038 [PMID:21366266]
NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membranes	B	6.87	pKi	134	nM	Ki	Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells	B	6.89	pKi	130	nM	Ki	J Med Chem (2008) 51: 1369-1376 [PMID:18266313]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane by liquid scintillation counting	B	6.89	pKi	130	nM	Ki	J Med Chem (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane	B	6.89	pKi	130	nM	Ki	J Med Chem (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells	B	6.89	pKi	130	nM	Ki	J Med Chem (2011) 54: 2029-2038 [PMID:21366266]
GtoPdb	-	-	6.34	pIC50	~460	nM	IC50	J Biol Chem (1994) 269: 6587-91 [PMID:7509807]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane by liquid scintillation counting	B	6.4	pIC50	398.11	nM	IC50	J Med Chem (2008) 51: 6334-6347 [PMID:18821747]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membrane	B	6.4	pIC50	398.11	nM	IC50	J Med Chem (2009) 52: 5164-5175 [PMID:20560643]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cell membranes	B	6.4	pIC50	398.11	nM	IC50	Bioorg Med Chem (2009) 17: 7337-7343 [PMID:19762245]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells	B	6.4	pIC50	398.11	nM	IC50	J Med Chem (2011) 54: 2029-2038 [PMID:21366266]
ChEMBL	Displacement of [3H]substance P from rat NK1 receptor expressed in CHO cells	B	6.4	pIC50	-6.4	-	logIC50	J Med Chem (2008) 51: 1369-1376 [PMID:18266313]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL	Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined	B	5.3	pIC50	>5000	nM	IC50	Bioorg Med Chem Lett (1998) 8: 2259-2262 [PMID:9873524]
ChEMBL	Binding affinity to the NK2 receptor assayed by displacement of [125I]-Neurokinin A	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (1994) 37: 1269-1274 [PMID:7513763]
Neurokinin 2 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3433] [UniProtKB: P79218]
ChEMBL	Antagonistic potency for NK-2 receptor was determined in vitro, using isolated rabbit pulmonary artery.	F	5.2	pKd	6309.57	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL	Displacement of [3H]substance P frome rat NK2 receptor	B	6.87	pKi	134	nM	Ki	J Med Chem (2010) 53: 5491-5501 [PMID:20617791]
ChEMBL	Displacement of [3H]substance P frome rat NK2 receptor	B	6.4	pIC50	398.11	nM	IC50	J Med Chem (2010) 53: 5491-5501 [PMID:20617791]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
ChEMBL	Affinity to NK3 receptors assayed by displacement of [125I]-Bolton-Hunter labeled eledoisin radioligand	B	5.3	pIC50	>5000	nM	IC50	J Med Chem (1994) 37: 1269-1274 [PMID:7513763]
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
ChEMBL	Antagonistic potency for NK-3 receptor was determined in vitro, using isolated rat portal vein.	F	5.2	pKd	6309.57	nM	Kd	Bioorg Med Chem Lett (1997) 7: 203-208

ChEMBL data shown on this page come from version 32:

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]