GPCRdb

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Ligand source activities (1 row/activity)

Affinity
Potency

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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-helical CRF	360	None	0	Human	Binding	pKd	None	-	7.55	-31	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9918582
5-Chloro-N-cyclopropylmethyl-N'-(2,6-dichloro-4-tributylstannanyl-phenyl)-2-methyl-N-propyl-pyrimidine-4,6-diamine	10161	None	0	Rat	Binding	Ki	=	3.00	8.52	-	1	Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(00)00661-2
antalarmin	426	None	22	Human	Binding	pKi	=	-	8.65	-1	2	Unclassified	Guide to Pharmacology	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://pubmed.ncbi.nlm.nih.gov/8940412
antalarmin	426	125I-Sauvagine	22	Human	Binding	pKi	=	3.10	8.51	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	125I-Astressin + GTP GammaS	22	Human	Binding	pKi	=	8.51	8.07	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	3H-NBI 35965 + GTP GammaS	22	Human	Binding	pKi	=	0.60	9.22	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	125I-Sauvigine + GTP GammaS	22	Human	Binding	pKi	=	1.95	8.71	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	125I-Sauvagine	22	Human	Binding	pKi	=	0.38	9.42	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	125I-Sauvagine	22	Human	Binding	pKi	=	3.10	8.51	-1	2	-	PDSP KiDatabase	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	-
antalarmin	426	None	22	Human	Binding	IC50	=	18.62	7.73	-1	2	Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1016/j.ejmech.2017.07.016
antalarmin	426	None	22	Human	Binding	IC50	=	18.62	7.73	-1	2	Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1016/j.ejmech.2014.03.040
antalarmin	426	None	22	Human	Binding	Ki	=	2.51	8.60	-1	2	Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1021/jm049085v
antalarmin	426	None	22	Human	Binding	Ki	=	3.10	8.51	-1	2	Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1021/jm050070m
antalarmin	426	None	22	Human	Binding	Ki	=	3.10	8.51	-1	2	Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1021/jm050384+
antalarmin	426	None	22	Human	Binding	Ki	=	0.84	9.08	-1	2	Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1021/jm980224g
antalarmin	426	None	22	Rat	Binding	Ki	=	1.00	9.00	1	2	Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1021/jm034077k
antalarmin	426	None	22	Rat	Binding	Ki	=	2.50	8.60	1	2	Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1016/s0960-894x(00)00071-8
astressin	506	None	0	Human	Binding	pKd	=	-	8.25	-3	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9851694
astressin	506	None	0	Human	Binding	pKd	=	-	8.25	-3	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11123370
astressin	506	None	0	Human	Binding	pKd	=	-	8.25	-3	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9918582

Showing 1 to 20 of 2,540 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

antalarmin	426	None	22	Human	Functional	Ki	=	32.00	7.50	-	2	Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay	ChEMBL	378.3	6	0	4	5.90	CCCCN(CC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C	https://dx.doi.org/10.1016/j.bmcl.2011.10.066
astressin	506	None	0	Human	Functional	pIC50	=	-	9.14	-1	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12361401
astressin 2B	507	None	0	Human	Functional	pIC50	>	-	6.30	-389	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12361401
CHEMBL10080	4302	None	0	Human	Functional	Ki	=	23.10	7.64	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	512.0	6	1	7	5.90	COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2[N+](=O)[O-])c(OC)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10082	4306	None	0	Human	Functional	Ki	=	5.50	8.26	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	478.1	5	0	4	6.91	CCN(c1nc(C)nc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)C)cc1Br	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10090	4325	None	0	Human	Functional	Ki	=	95.50	7.02	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	522.1	4	0	7	4.89	COc1cc(Br)c(-n2c(=O)n(C)c3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10091	4327	None	0	Human	Functional	Ki	=	60.30	7.22	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	482.1	5	2	6	5.58	COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2N)c(OC)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10142	4404	None	0	Human	Functional	Ki	=	32.30	7.49	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	506.1	4	0	6	5.90	COc1cc(Br)c(-n2c(C)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10154	4428	None	0	Human	Functional	Ki	=	2.00	8.70	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	398.1	6	1	4	6.03	CCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10174	4461	None	0	Human	Functional	Ki	=	33.40	7.48	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	502.0	3	0	5	7.49	CSc1nn(-c2c(Cl)cc(Cl)cc2Cl)c2nc(C)nc(-c3ccccc3C(F)(F)F)c12	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10279	4609	None	0	Human	Functional	Ki	=	202.00	6.70	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	508.0	4	1	7	5.29	COc1cc(Br)c(-n2c(O)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10315	4663	None	0	Human	Functional	Ki	=	168.00	6.78	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	397.2	2	0	5	5.13	Cc1cc(C)c(-n2nnc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(C)c1	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL10504	5009	None	0	Human	Functional	Ki	=	3.70	8.43	-	1	Antagonistic activity for Corticotropin releasing factor receptor 1	ChEMBL	462.1	9	0	8	3.50	COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br	https://dx.doi.org/10.1016/s0960-894x(99)00133-x
CHEMBL1077301	210950	None	0	Human	Functional	EC50	=	9.70	8.01	-8	3	Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay	ChEMBL	-	-	-	-	-	CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O	https://dx.doi.org/10.1021/jm990590f
CHEMBL111665	9420	None	0	Human	Functional	IC50	=	16.00	7.80	-	1	Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production	ChEMBL	390.1	6	0	4	5.88	CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12	https://dx.doi.org/10.1016/s0960-894x(03)00622-x
CHEMBL111665	9420	None	0	Human	Functional	IC50	=	16.00	7.80	-	1	Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production	ChEMBL	390.1	6	0	4	5.88	CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12	https://dx.doi.org/10.1016/s0960-894x(03)00621-8
CHEMBL112290	9545	None	0	Human	Functional	IC50	=	15.00	7.82	-	1	Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production	ChEMBL	392.1	6	0	5	4.72	CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12	https://dx.doi.org/10.1016/s0960-894x(03)00622-x
CHEMBL113097	9697	None	0	Human	Functional	IC50	=	51.00	7.29	-	1	Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production	ChEMBL	386.1	6	0	2	7.14	CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12	https://dx.doi.org/10.1016/s0960-894x(03)00684-x
CHEMBL115142	10040	None	0	Human	Functional	IC50	=	5.00	8.30	-	1	Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production	ChEMBL	418.2	8	0	4	6.66	CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12	https://dx.doi.org/10.1016/s0960-894x(03)00622-x
CHEMBL115142	10040	None	0	Human	Functional	IC50	=	15.80	7.80	-	1	Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production	ChEMBL	418.2	8	0	4	6.66	CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12	https://dx.doi.org/10.1016/s0960-894x(03)00621-8

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Ligand source activities (1 row/activity)