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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 | |
| AZD5069 | 548 | None | 40 | Human | Binding | pIC50 | = | - | 6.90 | -1 | 2 | Measuring displacement of CXCL8 binding to recombinant CXCR1 in HEK cell membrane preparations. | Guide to Pharmacology | 476.1 | 10 | 3 | 8 | 1.53 | C[C@@H](Oc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(F)c2F)n1)[C@@H](O)CO | https://pubmed.ncbi.nlm.nih.gov/25736418 | |
| AZD5069 | 548 | None | 40 | Human | Binding | Kd | = | 0.40 | 9.40 | -1 | 2 | Binding affinity to CXCL1 (unknown origin) expressed in human Polymorphonuclear neutrophil cells | ChEMBL | 476.1 | 10 | 3 | 8 | 1.53 | C[C@@H](Oc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(F)c2F)n1)[C@@H](O)CO | https://dx.doi.org/10.1021/acs.jmedchem.3c00849 | |
| CHEMBL1162935 | 10414 | None | 0 | Human | Binding | IC50 | = | 3058.00 | 5.51 | - | 2 | Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells | ChEMBL | 379.2 | 6 | 3 | 6 | 2.61 | C[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccc1 | https://dx.doi.org/10.1021/jm0609622 | |
| CHEMBL1188250 | 12814 | None | 0 | Human | Binding | IC50 | = | 30000.00 | 4.52 | - | 2 | Concentration required to inhibit [125I]-IL-8 binding towards C-X-C chemokine receptor type 1 of human expressed in CHO cells | ChEMBL | 369.0 | 3 | 4 | 3 | 3.91 | NCc1c(Cl)ccc(NC(=O)Nc2ccccc2Br)c1O | https://dx.doi.org/10.1016/j.bmcl.2004.06.097 | |
| CHEMBL182361 | 65090 | None | 0 | Human | Binding | IC50 | = | 3100.00 | 5.51 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 312.1 | 5 | 0 | 4 | 4.05 | CN(C)COc1ccc(-c2cc(-c3ccc(F)cc3)on2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183061 | 65535 | None | 0 | Human | Binding | IC50 | = | 2700.00 | 5.57 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 328.1 | 5 | 0 | 4 | 4.56 | CN(C)COc1ccc(-c2cc(-c3ccc(Cl)cc3)on2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183222 | 65607 | None | 0 | Human | Binding | IC50 | = | 4317.00 | 5.37 | - | 2 | Concentration required to inhibit [125I]-IL-8 binding towards C-X-C chemokine receptor type 1 of human expressed in CHO cells | ChEMBL | 447.0 | 4 | 3 | 4 | 3.70 | CN(C)S(=O)(=O)c1c(Cl)ccc(NC(=O)Nc2ccccc2Br)c1O | https://dx.doi.org/10.1016/j.bmcl.2004.06.097 | |
| CHEMBL183425 | 65681 | None | 0 | Human | Binding | IC50 | = | 2000.00 | 5.70 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 395.2 | 7 | 0 | 5 | 4.16 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(F)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183537 | 65879 | None | 0 | Human | Binding | IC50 | = | 11500.00 | 4.94 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 350.2 | 5 | 0 | 6 | 2.99 | CN1CCN(COc2ccc(-c3cc(-c4ccccn4)on3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183561 | 65886 | None | 0 | Human | Binding | IC50 | = | 22700.00 | 4.64 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 469.2 | 9 | 0 | 6 | 5.82 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(Oc5ccccc5)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183819 | 66104 | None | 5 | Human | Binding | IC50 | = | 6700.00 | 5.17 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 322.2 | 7 | 0 | 4 | 4.34 | CN(C)CCCOc1ccc(-c2cc(-c3ccccc3)no2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184185 | 66171 | None | 1 | Human | Binding | IC50 | = | 6037.00 | 5.22 | - | 2 | Concentration required to inhibit [125I]-IL-8 binding towards C-X-C chemokine receptor type 1 of human expressed in CHO cells | ChEMBL | 383.0 | 3 | 4 | 3 | 3.55 | NC(=O)c1c(Cl)ccc(NC(=O)Nc2ccccc2Br)c1O | https://dx.doi.org/10.1016/j.bmcl.2004.06.097 | |
| CHEMBL184318 | 66196 | None | 0 | Human | Binding | IC50 | = | 1600.00 | 5.80 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 383.1 | 5 | 0 | 5 | 4.25 | CN1CCN(COc2ccc(-c3cc(-c4ccc(Cl)cc4)on3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184319 | 66197 | None | 0 | Human | Binding | IC50 | = | 5400.00 | 5.27 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 334.2 | 5 | 0 | 4 | 4.83 | c1ccc(-c2cc(-c3ccc(OCN4CCCCC4)cc3)no2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184401 | 66216 | None | 0 | Human | Binding | IC50 | = | 12100.00 | 4.92 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 339.1 | 6 | 0 | 6 | 3.81 | CN(C)COc1ccc(-c2cc(-c3ccc([N+](=O)[O-])cc3)on2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184583 | 66264 | None | 0 | Human | Binding | IC50 | = | 8100.00 | 5.09 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 328.1 | 5 | 0 | 4 | 4.56 | CN(C)COc1cccc(-c2cc(-c3ccc(Cl)cc3)on2)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184637 | 66279 | None | 0 | Human | Binding | IC50 | = | 22.00 | 7.66 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 322.0 | 2 | 4 | 3 | 3.50 | O=C(Nc1ccc(O)cc1O)Nc1ccccc1Br | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL184882 | 66331 | None | 0 | Human | Binding | IC50 | = | 10500.00 | 4.98 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 396.2 | 7 | 0 | 6 | 3.56 | CN1CCN(CCCOc2ccc(-c3nc(-c4ccc(F)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL185176 | 66407 | None | 0 | Human | Binding | IC50 | = | 7600.00 | 5.12 | - | 1 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand | ChEMBL | 348.2 | 5 | 0 | 4 | 4.73 | CN1CCC(COc2ccc(-c3cc(-c4ccccc4)on3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL185259 | 66612 | None | 0 | Human | Binding | IC50 | = | 13360.00 | 4.87 | - | 2 | Concentration required to inhibit [125I]-IL-8 binding towards C-X-C chemokine receptor type 1 of human expressed in CHO cells | ChEMBL | 373.9 | 2 | 3 | 2 | 5.11 | O=C(Nc1ccccc1Br)Nc1ccc(Cl)c(Cl)c1O | https://dx.doi.org/10.1016/j.bmcl.2004.06.097 | |
Showing 1 to 20 of 341 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 | |
| CHEMBL182361 | 65090 | None | 0 | Human | Functional | IC50 | = | 4000.00 | 5.40 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophils | ChEMBL | 312.1 | 5 | 0 | 4 | 4.05 | CN(C)COc1ccc(-c2cc(-c3ccc(F)cc3)on2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL183425 | 65681 | None | 0 | Human | Functional | IC50 | = | 3800.00 | 5.42 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophils | ChEMBL | 395.2 | 7 | 0 | 5 | 4.16 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(F)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL3426944 | 119147 | None | 5 | Human | Functional | IC50 | = | 31.00 | 7.51 | 1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 466.1 | 7 | 3 | 6 | 3.34 | O=C(Nc1ccc(F)cc1)c1ccc(SCc2cc(OC(F)(F)F)ccc2B(O)O)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609002 | 123070 | None | 0 | Human | Functional | IC50 | = | 611.00 | 6.21 | 1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 365.1 | 6 | 4 | 5 | 1.76 | O=C(Nc1ccc(F)cc1)c1ccc(NCc2cccc(B(O)O)c2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609003 | 123071 | None | 0 | Human | Functional | IC50 | = | 4100.00 | 5.39 | -10 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 379.1 | 6 | 3 | 5 | 1.79 | CN(Cc1cccc(B(O)O)c1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609004 | 123072 | None | 0 | Human | Functional | IC50 | = | 4300.00 | 5.37 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 365.1 | 6 | 4 | 5 | 1.76 | O=C(Nc1ccc(F)cc1)c1ccc(NCc2ccc(B(O)O)cc2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609005 | 123073 | None | 0 | Human | Functional | IC50 | = | 1400.00 | 5.85 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 379.1 | 6 | 3 | 5 | 1.79 | CN(Cc1ccc(B(O)O)cc1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609006 | 123074 | None | 0 | Human | Functional | IC50 | = | 1700.00 | 5.77 | -20 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 380.1 | 6 | 3 | 6 | 1.18 | CN(Cc1ccc(B(O)O)cn1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609008 | 123075 | None | 0 | Human | Functional | IC50 | = | 1340.00 | 5.87 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 366.1 | 6 | 4 | 6 | 1.16 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2cccc(B(O)O)c2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609009 | 123076 | None | 0 | Human | Functional | IC50 | = | 2500.00 | 5.60 | 1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 380.1 | 6 | 3 | 6 | 1.18 | CN(Cc1cccc(B(O)O)c1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609010 | 123077 | None | 0 | Human | Functional | IC50 | = | 1700.00 | 5.77 | 1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 366.1 | 6 | 4 | 6 | 1.16 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2ccc(B(O)O)cc2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609011 | 123078 | None | 0 | Human | Functional | IC50 | = | 681.00 | 6.17 | -5 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 380.1 | 6 | 3 | 6 | 1.18 | CN(Cc1ccc(B(O)O)cc1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609012 | 123079 | None | 0 | Human | Functional | IC50 | = | 1700.00 | 5.77 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 381.1 | 6 | 3 | 7 | 0.58 | CN(Cc1ccc(B(O)O)cn1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609013 | 123080 | None | 0 | Human | Functional | IC50 | = | 326.00 | 6.49 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 456.2 | 8 | 3 | 6 | 2.75 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609016 | 123083 | None | 0 | Human | Functional | IC50 | = | 3.30 | 8.48 | 6 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 446.2 | 8 | 3 | 7 | 2.35 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609018 | 123084 | None | 0 | Human | Functional | IC50 | = | 7.00 | 8.15 | -1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 457.2 | 8 | 3 | 7 | 2.15 | O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609019 | 123085 | None | 0 | Human | Functional | IC50 | = | 2050.00 | 5.69 | 2 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 458.2 | 8 | 3 | 8 | 1.54 | O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL3609021 | 123086 | None | 0 | Human | Functional | IC50 | = | 444.00 | 6.35 | 1 | 2 | Antagonist activity at CXCR1 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis | ChEMBL | 447.2 | 8 | 3 | 8 | 1.74 | O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 | https://dx.doi.org/10.1016/j.bmcl.2015.07.090 | |
| CHEMBL365008 | 126297 | None | 0 | Human | Functional | IC50 | = | 3600.00 | 5.44 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophils | ChEMBL | 411.2 | 7 | 0 | 5 | 4.68 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(Cl)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
| CHEMBL365671 | 127218 | None | 0 | Human | Functional | IC50 | = | 4500.00 | 5.35 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophils | ChEMBL | 412.2 | 7 | 0 | 6 | 4.07 | CN1CCN(CCCOc2ccc(-c3nc(-c4ccc(Cl)cc4)no3)cc2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2004.05.080 | |
Showing 1 to 20 of 46 entries