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Ligand source activities (1 row/activity)
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 | |
4-Cl-cinnamoyl-c[DCys-4Pal-DTrp-Orn-Val-Cys]-His-amide | 115 | None | 0 | Human | Binding | pKd | = | - | 8.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12535707 | |
[Bz-Phe6]U-II (human) | 761 | None | 0 | Human | Binding | pKi | None | - | 9.10 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12495432 | |
[Cha6]U-II-(4-11) | 907 | None | 0 | Rat | Binding | pKi | = | - | 6.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17125276 | |
[Orn5]URP | 2967 | None | 0 | Rat | Binding | pKi | = | - | 7.17 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/18082287 | |
[Pen5]U-(4-11) (human) | 3042 | None | 0 | Human | Binding | pKi | = | - | 9.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12238917 | |
AC-7954 | 244 | None | 10 | Human | Binding | pKi | = | - | 6.60 | - | 2 | Unclassified | Guide to Pharmacology | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://pubmed.ncbi.nlm.nih.gov/12408704 | |
AC-7954 | 244 | None | 10 | Human | Binding | pKi | = | - | 6.60 | - | 2 | Unclassified | Guide to Pharmacology | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://pubmed.ncbi.nlm.nih.gov/15781415 | |
AC-7954 | 244 | None | 10 | Human | Binding | EC50 | = | 251.19 | 6.60 | - | 2 | Potency against human Urotensin 2 receptor | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm025551+ | |
AC-7954 | 244 | None | 10 | Human | Binding | EC50 | = | 1122.02 | 5.95 | - | 2 | Activity against human urotensin-2 receptor expressed in NIH3T3 cells | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm051121i | |
AC-7954 | 244 | None | 10 | Human | Binding | EC50 | = | 316.23 | 6.50 | - | 2 | Potency against human Urotensin 2 receptor | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm025551+ | |
AC-7954 | 244 | None | 10 | Rat | Binding | EC50 | = | 199.53 | 6.70 | - | 2 | Potency against rat Urotensin 2 receptor | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm025551+ | |
BIM 23127 | 649 | None | 0 | Human | Binding | pKd | None | - | 6.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12770925 | |
CHEMBL1163360 | 10429 | None | 1 | Human | Binding | IC50 | = | 67.00 | 7.17 | - | 1 | Binding affinity to human urotensin 2 receptor | ChEMBL | 560.3 | 9 | 2 | 5 | 6.19 | COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163463 | 210978 | None | 6 | Rat | Binding | Ki | = | 0.19 | 9.72 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163471 | 210980 | None | 0 | Rat | Binding | Ki | = | 17.00 | 7.77 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163475 | 210982 | None | 0 | Rat | Binding | Ki | = | 200.00 | 6.70 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163477 | 210983 | None | 0 | Rat | Binding | Ki | = | 610.00 | 6.21 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163479 | 210984 | None | 0 | Rat | Binding | Ki | = | 1100.00 | 5.96 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1164523 | 10466 | None | 0 | Human | Binding | Ki | = | 12.00 | 7.92 | 50 | 2 | Binding affinity to human urotensin 2 receptor | ChEMBL | 536.3 | 12 | 2 | 6 | 4.38 | CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165794 | 210991 | None | 0 | Rat | Binding | Ki | = | 15.00 | 7.82 | - | 1 | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u |
Showing 1 to 20 of 802 entries
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 | |
[3-iodo-Tyr6]U-II-(4-11) (human) | 103 | None | 0 | Human | Functional | pEC50 | = | - | 8.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12943190 | |
AC-7954 | 244 | None | 10 | Human | Functional | EC50 | = | 1122.02 | 5.95 | -2 | 2 | Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1016/j.bmc.2010.04.041 | |
AC-7954 | 244 | None | 10 | Human | Functional | EC50 | = | 250.00 | 6.60 | -2 | 2 | Agonist activity at human urotensin 2 expressed in CHO cells by FLIPR | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm901294u | |
AC-7954 | 244 | None | 10 | Human | Functional | EC50 | = | 300.00 | 6.52 | -2 | 2 | Agonist activity for human Urotensin 2 receptor | ChEMBL | 329.1 | 4 | 0 | 3 | 3.90 | CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 | https://dx.doi.org/10.1021/jm049110x | |
CHEMBL1163460 | 210977 | None | 0 | Rat | Functional | EC50 | = | 0.16 | 9.80 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163463 | 210978 | None | 6 | Rat | Functional | EC50 | = | 0.17 | 9.77 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163467 | 210979 | None | 0 | Rat | Functional | EC50 | = | 0.29 | 9.54 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163471 | 210980 | None | 0 | Rat | Functional | EC50 | = | 2.10 | 8.68 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163473 | 210981 | None | 0 | Rat | Functional | EC50 | = | 0.76 | 9.12 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163475 | 210982 | None | 0 | Rat | Functional | EC50 | = | 31.00 | 7.51 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163477 | 210983 | None | 0 | Rat | Functional | EC50 | = | 26.00 | 7.58 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1163479 | 210984 | None | 0 | Rat | Functional | EC50 | = | 37.00 | 7.43 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1164523 | 10466 | None | 0 | Rat | Functional | Ki | = | 600.00 | 6.22 | - | 2 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR | ChEMBL | 536.3 | 12 | 2 | 6 | 4.38 | CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165145 | 10481 | None | 0 | Rat | Functional | Ki | = | 34.00 | 7.47 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | 449.3 | 5 | 0 | 5 | 4.66 | CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165734 | 210986 | None | 0 | Rat | Functional | EC50 | = | 0.11 | 9.96 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165735 | 210987 | None | 0 | Rat | Functional | EC50 | = | 0.60 | 9.22 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165764 | 210988 | None | 0 | Rat | Functional | EC50 | = | 6.50 | 8.19 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165767 | 210989 | None | 0 | Rat | Functional | EC50 | = | 0.40 | 9.40 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | C[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165793 | 210990 | None | 0 | Rat | Functional | EC50 | = | 1.60 | 8.80 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O | https://dx.doi.org/10.1021/jm901294u | |
CHEMBL1165794 | 210991 | None | 0 | Rat | Functional | EC50 | = | 1.60 | 8.80 | - | 1 | Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR | ChEMBL | - | - | - | - | - | CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O | https://dx.doi.org/10.1021/jm901294u |
Showing 1 to 20 of 415 entries