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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

2MeSADP	75	None	11	Human	Binding	pKi	=	-	9.20	10	5	Unclassified	Guide to Pharmacology	473.0	7	6	13	-1.02	CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/11196645
2MeSADP	75	None	11	Human	Binding	Ki	=	32.10	7.49	10	5	Displacement of [3H]-2MesADP from recombinant human P2Y12 transfected in HEK cell membrane assessed as inhibition constant	ChEMBL	473.0	7	6	13	-1.02	CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://dx.doi.org/10.1016/j.bmcl.2022.128837
ADP	288	None	48	Human	Binding	pKi	=	-	5.90	-	7	Unclassified	Guide to Pharmacology	427.0	6	6	12	-1.75	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O	https://pubmed.ncbi.nlm.nih.gov/11196645
AR-C67085	463	None	9	Human	Binding	pKd	=	-	8.20	-	2	Unclassified	Guide to Pharmacology	647.0	11	7	14	1.11	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/23495690
AR-C67085	463	None	9	Human	Binding	IC50	=	2.51	8.60	-	2	Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by turbidimetric method	ChEMBL	647.0	11	7	14	1.11	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://dx.doi.org/10.1016/j.bmcl.2016.04.030
AR-C67085	463	None	9	Human	Binding	Kd	=	4.57	8.34	-	2	Binding affinity to P2Y12 receptor expressed in human platelets from 0.047 to 50 nM	ChEMBL	647.0	11	7	14	1.11	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://dx.doi.org/10.1016/j.bmcl.2005.08.104
AZD1283	541	None	47	Human	Binding	pKi	=	-	8.00	281	3	Unclassified	Guide to Pharmacology	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://pubmed.ncbi.nlm.nih.gov/24670650
AZD1283	541	None	47	Human	Binding	pKi	=	-	8.00	281	3	Unclassified	Guide to Pharmacology	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://pubmed.ncbi.nlm.nih.gov/24215345
AZD1283	541	None	47	Human	Binding	IC50	=	3200.00	5.50	281	3	Antagonist activity P2Y12 receptor in human blood assessed as inhibition of ADP-induced platelet aggregation measured as residual platelet count after 5 mins by flow cytometric analysis	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	9.00	8.05	281	3	Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	44.00	7.36	281	3	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	22.00	7.66	281	3	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	14.00	7.85	281	3	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	9.00	8.05	281	3	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Binding	IC50	=	11.00	7.96	281	3	Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1021/jm400820m
AZD1283	541	None	47	Human	Binding	IC50	=	3200.00	5.50	281	3	Antagonist activity at P2Y12 receptor in human whole blood assessed as inhibition of ADP-induced platelet aggregation after 5 mins by residual platelet count assay	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1021/jm400820m
BX 667	759	None	9	Human	Binding	IC50	=	29.00	7.54	-	1	Displacement of [3H]-2-Mes-ADP from human P2Y12 receptor	ChEMBL	586.3	11	2	9	2.53	CCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)OCC)c3ccc(C)cc3n2)CC1	https://dx.doi.org/10.1016/j.bmcl.2016.04.030
BX 667	759	None	9	Human	Binding	IC50	=	129.90	6.89	-	1	Antagonist activity at human P2Y12	ChEMBL	586.3	11	2	9	2.53	CCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)OCC)c3ccc(C)cc3n2)CC1	https://dx.doi.org/10.1021/acs.jmedchem.5b01972
BX 667	759	None	9	Human	Binding	IC50	=	130.00	6.89	-	1	Antagonist activity at P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation measured for 5 mins by light transmission analysis	ChEMBL	586.3	11	2	9	2.53	CCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)OCC)c3ccc(C)cc3n2)CC1	https://dx.doi.org/10.1016/j.bmcl.2016.04.030
BX 667	759	None	9	Human	Binding	Ki	=	86.00	7.07	-	1	Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method	ChEMBL	586.3	11	2	9	2.53	CCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)OCC)c3ccc(C)cc3n2)CC1	https://dx.doi.org/10.1021/jm300771j

Showing 1 to 20 of 1,303 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

2MeSADP	75	None	11	Human	Functional	pIC50	=	-	8.55	-2	5	Unclassified	Guide to Pharmacology	473.0	7	6	13	-1.02	CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/11502873
2MeSAMP	76	None	0	Human	Functional	pIC50	=	-	5.40	-1	2	Unclassified	Guide to Pharmacology	393.1	5	5	11	-1.14	CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/11502873
2MeSATP	77	None	13	Rat	Functional	EC50	=	1.10	8.96	1	7	Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)	ChEMBL	553.0	9	7	15	-0.91	CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://dx.doi.org/10.1021/jm020046y
ADP	288	None	48	Rat	Functional	EC50	=	69.00	7.16	-1	7	Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)	ChEMBL	427.0	6	6	12	-1.75	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O	https://dx.doi.org/10.1021/jm020046y
ADPβS	289	None	12	Human	Functional	pIC50	=	-	8.60	32	6	Unclassified	Guide to Pharmacology	443.0	6	6	12	-1.63	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O	https://pubmed.ncbi.nlm.nih.gov/11502873
ADPβS	289	None	12	Rat	Functional	EC50	=	82.00	7.09	-32	6	Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)	ChEMBL	443.0	6	6	12	-1.63	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O	https://dx.doi.org/10.1021/jm020046y
ANAGRELIDE	207359	None	46	Human	Functional	EC50	=	1050.00	5.98	-	1	Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP)	ChEMBL	255.0	0	1	3	1.93	O=C1CN2Cc3c(ccc(Cl)c3Cl)N=C2N1	https://dx.doi.org/10.1021/jm00092a019
Ap₄A	450	None	0	Human	Functional	pIC50	=	-	6.00	-5	4	Unclassified	Guide to Pharmacology	832.0	14	6	29	-4.97	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O	https://pubmed.ncbi.nlm.nih.gov/12815166
AR-C67085	463	None	9	Human	Functional	EC50	=	1.30	8.89	38	2	The compound was evaluated for antagonist activity against phospholipase C coupled human P2Y purinoceptor 12 (P2Y12)	ChEMBL	647.0	11	7	14	1.11	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://dx.doi.org/10.1021/jm020046y
ARL66096	473	None	0	Human	Functional	pIC50	=	-	7.95	-	1	Unclassified	Guide to Pharmacology	615.0	11	7	14	0.58	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/7582510
ARL66096	473	None	0	Human	Functional	pIC50	=	-	7.95	-	1	Unclassified	Guide to Pharmacology	615.0	11	7	14	0.58	CCCSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]3O)c2n1	https://pubmed.ncbi.nlm.nih.gov/7858849
ATP	520	None	42	Rat	Functional	EC50	=	3190.00	5.50	-190	10	Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)	ChEMBL	507.0	8	7	14	-1.63	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O	https://dx.doi.org/10.1021/jm020046y
ATPGAMMAS	21755	None	12	Rat	Functional	EC50	=	1300.00	5.89	-2	4	Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12)	ChEMBL	523.0	8	7	14	-1.51	Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(O)(O)=S)[C@@H](O)[C@H]1O	https://dx.doi.org/10.1021/jm020046y
AZD1283	541	None	47	Human	Functional	IC50	=	3600.00	5.44	-	3	Antagonist activity at P2Y12 receptor in human platelet rich plasma	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmc.2022.116614
AZD1283	541	None	47	Human	Functional	IC50	=	25.00	7.60	-	3	Antagonist activity at P2Y12 receptor (unknown origin) assessed as inhibition of ADP-induced [35S]GTPgammaS binding after 45 mins by scintillation counting analysis	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1016/j.bmcl.2014.04.001
AZD1283	541	None	47	Human	Functional	IC50	=	25.00	7.60	-	3	Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay	ChEMBL	470.2	7	1	8	2.30	CCOC(=O)c1cc(C#N)c(N2CCC(C(=O)NS(=O)(=O)Cc3ccccc3)CC2)nc1C	https://dx.doi.org/10.1021/jm400820m
BX 048	757	None	0	Human	Functional	pIC50	=	-	6.50	-	1	Unclassified	Guide to Pharmacology	558.2	10	3	8	2.05	CCOC(=O)N1CCN(C(=O)C(CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)O)c3ccc(C)cc3n2)CC1	https://pubmed.ncbi.nlm.nih.gov/18539312
BX 667	759	None	9	Human	Functional	pIC50	None	-	7.00	-	1	Unclassified	Guide to Pharmacology	586.3	11	2	9	2.53	CCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2cc(OC(C)(C)C(=O)OCC)c3ccc(C)cc3n2)CC1	https://pubmed.ncbi.nlm.nih.gov/18539312
cangrelor	787	None	27	Human	Functional	pIC50	=	-	8.00	-2	4	Unclassified	Guide to Pharmacology	774.9	15	7	15	2.85	CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O	https://pubmed.ncbi.nlm.nih.gov/11502873
cangrelor	787	None	27	Human	Functional	pIC50	=	-	9.40	-2	4	Unclassified	Guide to Pharmacology	774.9	15	7	15	2.85	CSCCNc1nc(SCCC(F)(F)F)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O	https://pubmed.ncbi.nlm.nih.gov/12213051

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Ligand source activities (1 row/activity)