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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 | |
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) | 1478 | None | 0 | Human | Binding | pKi | = | - | 8.75 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10454496 | |
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) | 1478 | None | 0 | Human | Binding | pKi | = | - | 8.75 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/21729729 | |
[Leu8]-phyllolitorin | 2307 | None | 0 | Rat | Binding | pKi | > | - | 5.00 | -23 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9325344 | |
[Leu8]-phyllolitorin | 2307 | None | 0 | Rat | Binding | pKi | > | - | 5.00 | -23 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10353842 | |
[Phe13]bombesin | 3102 | None | 0 | Rat | Binding | pKi | = | - | 7.34 | -58 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10454496 | |
[Phe13]bombesin | 3102 | None | 0 | Rat | Binding | pKi | = | - | 7.34 | -58 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9325344 | |
[Phe13]bombesin | 3102 | None | 0 | Rat | Binding | pKi | = | - | 7.34 | -58 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10353842 | |
bag-1 | 569 | None | 23 | Human | Binding | IC50 | = | 7000.00 | 5.16 | - | 5 | Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human NMB-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting | ChEMBL | 333.2 | 7 | 1 | 2 | 5.24 | CCC(C)(C)Cc1cnc(CCc2ccc(-c3ccccn3)cc2)[nH]1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.076 | |
bombesin | 704 | None | 34 | Human | Binding | pKi | = | - | 7.48 | -7 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10454496 | |
bombesin | 704 | None | 34 | Human | Binding | pKi | = | - | 7.48 | -7 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7838118 | |
bombesin | 704 | None | 34 | Human | Binding | Ki | = | 2.00 | 8.70 | -7 | 6 | Binding affinity against [125 I][4Tyr]-bombesin labeled cloned human NMB receptor stably expressed in CHO cells | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/0960-894X(96)00481-7 | |
bombesin | 704 | None | 34 | Rat | Binding | pKi | = | - | 7.57 | -24 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10454496 | |
bombesin | 704 | None | 34 | Rat | Binding | pKi | = | - | 7.57 | -24 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7838118 | |
CHEMBL100065 | 4172 | None | 0 | Human | Binding | IC50 | = | 790.00 | 6.10 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 633.4 | 8 | 4 | 3 | 8.75 | Cc1ccc2[nH]c3c(c2c1)C(C)C(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL100065 | 4172 | None | 0 | Human | Binding | IC50 | = | 700.00 | 6.16 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 633.4 | 8 | 4 | 3 | 8.75 | Cc1ccc2[nH]c3c(c2c1)C(C)C(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL101026 | 4343 | None | 0 | Human | Binding | IC50 | = | 660.00 | 6.18 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 619.4 | 8 | 4 | 3 | 8.19 | Cc1cccc2[nH]c3c(c12)CC(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL102647 | 4590 | None | 0 | Human | Binding | IC50 | = | 2140.00 | 5.67 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 683.3 | 8 | 4 | 3 | 8.64 | CC(C)c1cccc(C(C)C)c1NC(=O)NC1(C(=O)NCC2(c3ccccn3)CCCCC2)CCc2[nH]c3cc(Br)ccc3c2C1 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL103430 | 4697 | None | 0 | Human | Binding | IC50 | = | 3660.00 | 5.44 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 673.4 | 8 | 4 | 3 | 8.90 | CC(C)c1cccc(C(C)C)c1NC(=O)NC1(C(=O)NCC2(c3ccccn3)CCCCC2)CCc2[nH]c3cccc(C(F)(F)F)c3c2C1 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL103439 | 4699 | None | 0 | Human | Binding | IC50 | = | 620.00 | 6.21 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 580.3 | 7 | 4 | 5 | 5.85 | Cc1cc([N+](=O)[O-])ccc1NC(=O)NC1(C(=O)NCC2(c3ccccn3)CCCCC2)CCc2[nH]c3ccccc3c2C1 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL103440 | 4700 | None | 0 | Human | Binding | IC50 | = | 800.00 | 6.10 | - | 1 | Affinity of [125I][D-Tyr0]-NMB to human Neuromedin B receptor expressed in HEK293 cells | ChEMBL | 566.3 | 7 | 4 | 5 | 5.54 | O=C(Nc1ccc([N+](=O)[O-])cc1)NC1(C(=O)NCC2(c3ccccn3)CCCCC2)CCc2[nH]c3ccccc3c2C1 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 |
Showing 1 to 20 of 183 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 | |
[D-Phe6, Leu13, Cpa14,ψ13-14]bombesin-(6-14) | 1481 | None | 0 | Human | Functional | pIC50 | > | - | 5.00 | -7762 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/19463875 | |
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) | 1478 | None | 0 | Human | Functional | pIC50 | = | - | 9.59 | -4 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/21729729 | |
[Leu8]-phyllolitorin | 2307 | None | 0 | Human | Functional | pIC50 | = | - | 6.52 | -2 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | - | |
[Leu8]-phyllolitorin | 2307 | None | 0 | Rat | Functional | pIC50 | = | - | 6.84 | -1 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/21729729 | |
bantag-1 | 573 | None | 0 | Human | Functional | pIC50 | = | - | 5.24 | -3388 | 5 | Unclassified | Guide to Pharmacology | 894.6 | 23 | 7 | 8 | 4.76 | CC(C)C[C@H](NC(=O)C[C@H](O)[C@H](CC1CCCCC1)NC(O)[C@H](Cc1c[nH]c[nH+]1)N(C)C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C(=O)NCC1=CCCC(C[N+](C)(C)C)=C1 | https://pubmed.ncbi.nlm.nih.gov/20096642 | |
bantag-1 | 573 | None | 0 | Human | Functional | pIC50 | = | - | 5.24 | -3388 | 5 | Unclassified | Guide to Pharmacology | 894.6 | 23 | 7 | 8 | 4.76 | CC(C)C[C@H](NC(=O)C[C@H](O)[C@H](CC1CCCCC1)NC(O)[C@H](Cc1c[nH]c[nH+]1)N(C)C(=O)[C@H](CC1=CC=CCC1)NC(=O)OC(C)(C)C)C(=O)NCC1=CCCC(C[N+](C)(C)C)=C1 | https://pubmed.ncbi.nlm.nih.gov/23892571 | |
bombesin | 704 | None | 34 | Human | Functional | Ki | = | 2.00 | 8.70 | -6 | 6 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
bombesin | 704 | None | 34 | Human | Functional | pIC50 | = | - | 8.59 | -6 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/21729729 | |
CHEMBL103756 | 4747 | None | 0 | Human | Functional | EC50 | = | 1970.00 | 5.71 | - | 1 | Agonistic activity was determined against human Neuromedin B receptor transfected in HEK293 cells as accumulation levels of inositol phosphate | ChEMBL | 635.4 | 9 | 4 | 4 | 7.89 | COc1cccc2[nH]c3c(c12)CC(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL103756 | 4747 | None | 0 | Human | Functional | EC50 | = | 132.00 | 6.88 | - | 1 | Agonistic activity was determined against human Neuromedin B receptor transfected in HEK293 cells as accumulation levels of inositol phosphate | ChEMBL | 635.4 | 9 | 4 | 4 | 7.89 | COc1cccc2[nH]c3c(c12)CC(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL103756 | 4747 | None | 0 | Human | Functional | EC50 | = | 17.70 | 7.75 | - | 1 | Agonistic activity was determined against human Neuromedin B receptor transfected in HEK293 cells as accumulation levels of inositol phosphate | ChEMBL | 635.4 | 9 | 4 | 4 | 7.89 | COc1cccc2[nH]c3c(c12)CC(NC(=O)Nc1c(C(C)C)cccc1C(C)C)(C(=O)NCC1(c2ccccn2)CCCCC1)CC3 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 | |
CHEMBL262992 | 96612 | None | 0 | Human | Functional | EC50 | = | 310.00 | 6.51 | -3 | 3 | Effective concentration required against nueromedin B receptor (NMB-R) in CHO cells by using FLIPR assay | ChEMBL | 1105.6 | 31 | 11 | 12 | 2.10 | CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)O | https://dx.doi.org/10.1021/jm0210921 | |
CHEMBL312926 | 106007 | None | 0 | Human | Functional | Ki | = | 0.46 | 9.34 | - | 2 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | 583.3 | 10 | 4 | 5 | 6.23 | COc1ccc(C2(CNC(=O)[C@](C)(Cc3c[nH]c4ccccc34)NC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)cc1 | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
CHEMBL313030 | 106028 | None | 0 | Human | Functional | Ki | = | 1.50 | 8.82 | - | 2 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | 595.3 | 10 | 4 | 4 | 7.34 | CC(C)c1ccc(C2(CNC(=O)[C@](C)(Cc3c[nH]c4ccccc34)NC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)cc1 | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
CHEMBL313346 | 106122 | None | 0 | Human | Functional | Ki | = | 0.97 | 9.01 | - | 2 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | 554.3 | 9 | 4 | 5 | 5.61 | C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)Nc1cccc([N+](=O)[O-])c1)C(=O)NCC1(c2ccccn2)CCCCC1 | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
CHEMBL314375 | 213639 | None | 0 | Human | Functional | Ki | = | 2.10 | 8.68 | - | 2 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(C)=O)C(C)C)C(N)=O | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
CHEMBL3144498 | 106842 | None | 0 | Human | Functional | EC50 | = | 18500.00 | 4.73 | -13 | 3 | Effective concentration required against nueromedin B receptor (NMB-R) in CHO cells by using FLIPR assay | ChEMBL | 587.2 | 14 | 5 | 4 | 3.20 | NC(=O)CC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 | https://dx.doi.org/10.1021/jm0210921 | |
CHEMBL3144503 | 106847 | None | 0 | Human | Functional | EC50 | = | 15000.00 | 4.82 | -12 | 3 | Effective concentration required against nueromedin B receptor (NMB-R) in CHO cells by using FLIPR assay | ChEMBL | 553.3 | 14 | 5 | 4 | 2.55 | NC(=O)CC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccc1 | https://dx.doi.org/10.1021/jm0210921 | |
CHEMBL316085 | 107181 | None | 0 | Human | Functional | Ki | = | 2.80 | 8.55 | - | 2 | Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells | ChEMBL | 543.2 | 8 | 4 | 3 | 6.36 | C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(Cl)cc1)C(=O)NCC1(c2ccccn2)CCCCC1 | https://dx.doi.org/10.1016/s0960-894x(98)00462-4 | |
CHEMBL318548 | 107551 | None | 0 | Human | Functional | EC50 | = | 603.00 | 6.22 | - | 1 | Agonistic activity was determined against human Neuromedin B receptor transfected in HEK293 cells as accumulation levels of inositol phosphate | ChEMBL | 605.4 | 8 | 4 | 3 | 7.88 | CC(C)c1cccc(C(C)C)c1NC(=O)NC1(C(=O)NCC2(c3ccccn3)CCCCC2)CCc2[nH]c3ccccc3c2C1 | https://dx.doi.org/10.1016/j.bmcl.2004.04.045 |
Showing 1 to 20 of 62 entries