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Ligand source activities (1 row/activity)

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

α-methyl-5-HT	364	None	24	Human	Binding	Ki	=	150.00	6.82	-34	19	Binding affinity was determined against 5-hydroxytryptamine 1D receptor in bovine caudate homogenate	ChEMBL	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00164a046
α-methyl-5-HT	364	None	24	Human	Binding	pKi	None	-	6.35	-34	19	Unclassified	Guide to Pharmacology	190.1	2	3	2	1.76	CC(N)Cc1c[nH]c2ccc(O)cc12	https://pubmed.ncbi.nlm.nih.gov/8967979
(+)-WAY 100135	4070	None	6	Human	Binding	pKi	None	-	7.60	-19	5	Unclassified	Guide to Pharmacology	395.3	6	1	4	3.52	COc1ccccc1N1CCN(C[C@@H](C(=O)NC(C)(C)C)c2ccccc2)CC1	https://pubmed.ncbi.nlm.nih.gov/9208142
(-)-adrenaline	291	3H-5HT	40	Bovine	Binding	pKi	=	10000.00	5.00	-1862	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-pindolol	3126	3H-5HT	37	Human	Binding	pKi	=	10000.00	5.00	-20417	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Human	Binding	pKi	=	7800.00	5.11	-20417	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Bovine	Binding	pKi	=	7000.00	5.15	-14791	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Bovine	Binding	pKi	=	6310.00	5.20	-14791	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Bovine	Binding	pKi	=	5890.00	5.23	-14791	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Bovine	Binding	pKi	=	5890.00	5.23	-14791	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-pindolol	3126	3H-5HT	37	Bovine	Binding	pKi	=	5890.00	5.23	-14791	15	-	PDSP KiDatabase	248.2	6	3	3	1.91	CC(C)NC[C@H](O)COc1cccc2[nH]ccc12	-
(-)-propranolol	3187	None	44	Human	Binding	pKi	=	5.35	8.27	-11	34	None	Drug Central	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	-
(-)-stepholidine	3691	3H-GR-125743	40	Human	Binding	pKi	=	10000.00	5.00	-2290	35	-	PDSP KiDatabase	327.1	2	2	5	2.77	COc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2	-
(1R,2S)-PHENYLPROPANOLAMINE	27120	3H-GR-125743	13	Human	Binding	pKi	=	10000.00	5.00	-38	42	-	PDSP KiDatabase	151.1	2	2	2	1.07	C[C@H](N)[C@H](O)c1ccccc1	-
(R)-ZINC-3573	3426	None	17	Human	Binding	Ki	=	1698.24	5.77	-4	6	GPCRScan assay: inhibition of 5-HT1D	ChEMBL	307.2	3	0	5	2.54	CN(C)[C@@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1	https://dx.doi.org/10.6019/CHEMBL4507322
(R)-ZINC-3573	3426	None	17	Human	Binding	Ki	=	1744.10	5.76	-4	6	GPCRScan assay: inhibition of 5-HT1D	ChEMBL	307.2	3	0	5	2.54	CN(C)[C@@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1	https://dx.doi.org/10.6019/CHEMBL4507322
(S)-1-{2-[4-(4-Methoxy-phenyl)-piperazin-1-yl]-ethyl}-isochroman-6-carboxylic acid methylamide	219730	UNDEFINED	0	Human	Binding	pKi	=	0.90	9.05	-	1	-	PDSP KiDatabase	409.2	6	1	5	2.88	CNC(=O)c1ccc2c(c1)CCOC2CCN1CCN(c2ccc(OC)cc2)CC1	-
(S)-UH-301	218510	3H-8-OH-DPAT	0	Human	Binding	pKi	=	10000.00	5.00	-154	7	-	PDSP KiDatabase	265.2	5	1	2	3.51	CCCN(CCC)C1CCc2c(F)ccc(O)c2C1	-
(S)-ZINC-3573	216453	None	20	Human	Binding	Ki	=	2961.88	5.53	-2	3	GPCRScan assay: inhibition of 5-HT1D	ChEMBL	-	-	-	-	-	CN(C)[C@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1	https://dx.doi.org/10.6019/CHEMBL4507322
(S)-ZINC-3573	216453	None	20	Human	Binding	Ki	=	2884.03	5.54	-2	3	GPCRScan assay: inhibition of 5-HT1D	ChEMBL	-	-	-	-	-	CN(C)[C@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1	https://dx.doi.org/10.6019/CHEMBL4507322

Showing 1 to 20 of 2,467 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

5-(nonyloxy)-tryptamine	148	None	19	Human	Functional	ED50	=	68.00	7.17	234	7	Compound was evaluated for its agonistic activity on 5-hydroxytryptamine 1D receptor	ChEMBL	302.2	11	2	2	4.80	CCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1	https://dx.doi.org/10.1021/jm00044a001
5-(nonyloxy)-tryptamine	148	None	19	Human	Functional	EC50	=	68.00	7.17	234	7	Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1D-beta receptor in CHO-K1 cells	ChEMBL	302.2	11	2	2	4.80	CCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1	https://dx.doi.org/10.1016/0960-894X(95)00091-7
5-HT-moduline	138	None	0	Human	Functional	pIC50	None	-	12.00	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9774213
5-hydroxytryptamine	139	None	45	Human	Functional	ED50	=	1.20	8.92	-5	61	Compound was evaluated for its agonistic activity on 5-hydroxytryptamine 1D receptor	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00044a001
5-hydroxytryptamine	139	None	45	Human	Functional	Ki	=	5.06	8.30	-5	61	Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1D receptor in CHO-K1 cells	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm960552l
5-hydroxytryptamine	139	None	45	Guinea pig	Functional	EC50	=	5.20	8.28	-12	61	Effect on forskolin stimulated adenylate cyclase activity at 5-HT1D receptor of guinea pig substantia nigra.	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00101a032
5-hydroxytryptamine	139	None	45	Rat	Functional	EC50	=	5.20	8.28	-7	61	Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor	ChEMBL	176.1	2	3	2	1.38	NCCc1c[nH]c2ccc(O)cc12	https://dx.doi.org/10.1021/jm00042a003
CHEMBL111899	9466	None	0	Human	Functional	ED50	=	1.40	8.85	20	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	464.3	9	2	6	4.02	CN(CC1CCCCC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL112507	9593	None	0	Human	Functional	ED50	=	0.25	9.60	199	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	415.2	7	2	5	3.75	OC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL112558	9603	None	0	Human	Functional	ED50	=	3.20	8.49	16	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	445.3	9	3	7	2.69	OC1(CNCc2ccccn2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL114303	9897	None	0	Human	Functional	ED50	=	3.70	8.43	40	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	472.3	9	2	6	3.95	Cc1ccccc1CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL114877	9994	None	0	Human	Functional	ED50	=	3.80	8.42	44	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	458.3	9	2	6	3.64	CN(Cc1ccccc1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL115352	10074	None	0	Human	Functional	ED50	=	1.60	8.80	36	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	438.3	8	2	6	3.49	CN(CC(C)(C)C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL115496	10101	None	0	Human	Functional	ED50	=	9.70	8.01	23	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	454.3	7	3	7	3.03	CC(C)(C)OC(=O)NCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL115750	10145	None	0	Human	Functional	EC50	=	1.50	8.82	109	2	Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the human 5-hydroxytryptamine 1D receptor.	ChEMBL	432.2	8	1	5	3.68	Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1	https://dx.doi.org/10.1021/jm980569z
CHEMBL115750	10145	None	0	Human	Functional	EC50	=	1.50	8.82	109	2	Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing 5-hydroxytryptamine 1D receptor	ChEMBL	432.2	8	1	5	3.68	Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1	https://dx.doi.org/10.1021/jm9704560
CHEMBL115989	10204	None	0	Human	Functional	ED50	=	1.10	8.96	21	2	Measurement of agonist-induced [35S]-GTP gamma-S binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor	ChEMBL	422.3	9	2	6	2.85	CN(CC1CC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1016/s0960-894x(99)00614-9
CHEMBL116031	10224	None	0	Human	Functional	EC50	=	1.40	8.85	112	2	Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the human 5-hydroxytryptamine 1D receptor.	ChEMBL	432.2	8	1	5	3.68	Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1021/jm980569z
CHEMBL116031	10224	None	0	Human	Functional	EC50	=	1.50	8.82	112	2	Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing 5-hydroxytryptamine 1D receptor	ChEMBL	432.2	8	1	5	3.68	Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1	https://dx.doi.org/10.1021/jm9704560
CHEMBL116092	10246	None	0	Human	Functional	EC50	=	2.30	8.64	10	2	Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor	ChEMBL	281.2	4	1	4	2.39	c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1	https://dx.doi.org/10.1021/jm980569z

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Ligand source activities (1 row/activity)