Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 11372270 | 67525 | None | 26 | Human | Functional | pIC50 | = | 9.2 | 9.2 | -2 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1016/j.ejmech.2023.115175 | ||
| 11372270.0 | 67525 | None | 26 | Human | Functional | pIC50 | = | 9.2 | 9.2 | -2 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1016/j.ejmech.2023.115175 | ||
| CHEMBL189475 | 67525 | None | 26 | Human | Functional | pIC50 | = | 9.2 | 9.2 | -2 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1016/j.ejmech.2023.115175 | ||
| CHEMBL4442431 | 67525 | None | 26 | Human | Functional | pIC50 | = | 9.2 | 9.2 | -2 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1016/j.ejmech.2023.115175 | ||
| 12073810 | 171655 | None | 18 | Human | Functional | pIC50 | = | 9 | 9.0 | - | 1 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 384 | 6 | 3 | 7 | 2.7 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2[nH]c(=O)sc12 | 10.1016/j.ejmech.2023.115175 | ||
| CHEMBL446458 | 171655 | None | 18 | Human | Functional | pIC50 | = | 9 | 9.0 | - | 1 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 384 | 6 | 3 | 7 | 2.7 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2[nH]c(=O)sc12 | 10.1016/j.ejmech.2023.115175 | ||
| 8498 | 3315 | None | 44 | Human | Functional | pIC50 | = | 9 | 9.0 | -33 | 2 | Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| 9838712 | 3315 | None | 44 | Human | Functional | pIC50 | = | 9 | 9.0 | -33 | 2 | Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| 9838712.0 | 3315 | None | 44 | Human | Functional | pIC50 | = | 9 | 9.0 | -33 | 2 | Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| CHEMBL191413 | 3315 | None | 44 | Human | Functional | pIC50 | = | 9 | 9.0 | -33 | 2 | Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| DB12614 | 3315 | None | 44 | Human | Functional | pIC50 | = | 9 | 9.0 | -33 | 2 | Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| 135907804 | 113023 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay |
ChEMBL | 363 | 5 | 2 | 6 | 2.8 | N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(=O)O | 10.1016/j.bmcl.2014.06.011 | ||
| CHEMBL3310786 | 113023 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay |
ChEMBL | 363 | 5 | 2 | 6 | 2.8 | N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(=O)O | 10.1016/j.bmcl.2014.06.011 | ||
| 8497 | 2737 | None | 41 | Human | Functional | pIC50 | = | 8 | 8.0 | 1 | 4 | Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/acsmedchemlett.1c00113 | ||
| 9865554 | 2737 | None | 41 | Human | Functional | pIC50 | = | 8 | 8.0 | 1 | 4 | Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL216981 | 2737 | None | 41 | Human | Functional | pIC50 | = | 8 | 8.0 | 1 | 4 | Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/acsmedchemlett.1c00113 | ||
| 162646828 | 179716 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | 912 | 2 | Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 413 | 4 | 3 | 6 | 3.1 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C3CCCCC3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4742368 | 179716 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | 912 | 2 | Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 413 | 4 | 3 | 6 | 3.1 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C3CCCCC3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| 45485775 | 200141 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis |
ChEMBL | 424 | 8 | 3 | 8 | 2.3 | CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(OC)cc1 | 10.1016/j.bmcl.2009.08.014 | ||
| CHEMBL571141 | 200141 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis |
ChEMBL | 424 | 8 | 3 | 8 | 2.3 | CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(OC)cc1 | 10.1016/j.bmcl.2009.08.014 | ||
| 163322282 | 191744 | None | 3 | Human | Functional | pIC50 | = | 7 | 7.0 | 478 | 2 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 352 | 6 | 2 | 7 | 3.0 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2oncc12 | 10.1016/j.ejmech.2023.115240 | ||
| CHEMBL5195797 | 191744 | None | 3 | Human | Functional | pIC50 | = | 7 | 7.0 | 478 | 2 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 352 | 6 | 2 | 7 | 3.0 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2oncc12 | 10.1016/j.ejmech.2023.115240 | ||
| 24970094 | 126879 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's. |
ChEMBL | 397 | 8 | 2 | 4 | 3.6 | CC(C)(NC(=O)c1ccc2c(c1OCCOc1ccccc1)CCCC2)C(=O)O | nan | ||
| CHEMBL3654434 | 126879 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's. |
ChEMBL | 397 | 8 | 2 | 4 | 3.6 | CC(C)(NC(=O)c1ccc2c(c1OCCOc1ccccc1)CCCC2)C(=O)O | nan | ||
| 136074345 | 113029 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 1 | Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay |
ChEMBL | 319 | 4 | 1 | 5 | 3.5 | N#Cc1c(O)nc(CSc2cccc(F)c2F)nc1C1CC1 | 10.1016/j.bmcl.2014.06.011 | ||
| CHEMBL3310793 | 113029 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 1 | Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay |
ChEMBL | 319 | 4 | 1 | 5 | 3.5 | N#Cc1c(O)nc(CSc2cccc(F)c2F)nc1C1CC1 | 10.1016/j.bmcl.2014.06.011 | ||
| CHEMBL5083610 | 217363 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay |
ChEMBL | None | None | None | O=C(Nc1ccccc1F)Nc1ccc2c(c1O)S(=O)(=O)CCC2 | 10.1021/acs.jmedchem.1c01219 | ||||
| 1485055 | 35431 | None | 19 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 271 | 3 | 1 | 5 | 3.0 | Cc1cc2nc(CSc3ccccc3)cc(O)n2n1 | 10.1016/j.bmcl.2013.11.074 | ||
| CHEMBL1437942 | 35431 | None | 19 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 271 | 3 | 1 | 5 | 3.0 | Cc1cc2nc(CSc3ccccc3)cc(O)n2n1 | 10.1016/j.bmcl.2013.11.074 | ||
| 91937331 | 114993 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay |
ChEMBL | 380 | 6 | 4 | 6 | 2.0 | O=C(Nc1ccc(O)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 | 10.1021/jm500827t | ||
| CHEMBL3342318 | 114993 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay |
ChEMBL | 380 | 6 | 4 | 6 | 2.0 | O=C(Nc1ccc(O)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 | 10.1021/jm500827t | ||
| CHEMBL5076384 | 216922 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay |
ChEMBL | None | None | None | O=c1c(Nc2ccccc2Cl)c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c1=O | 10.1021/acs.jmedchem.1c01219 | ||||
| 72948072 | 104688 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 319 | 5 | 1 | 5 | 2.3 | COc1cc(CCc2cccc(F)c2F)nc2cc(CO)nn12 | 10.1016/j.bmcl.2013.11.074 | ||
| CHEMBL3104898 | 104688 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 319 | 5 | 1 | 5 | 2.3 | COc1cc(CCc2cccc(F)c2F)nc2cc(CO)nn12 | 10.1016/j.bmcl.2013.11.074 | ||
| 172458912 | 196325 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | Inhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assayInhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assay |
ChEMBL | 526 | 10 | 4 | 9 | 3.8 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)CCNC(=O)OC(C)(C)C)c2O)c(=O)c1=O)c1ccc(C)o1 | 10.1021/acs.jmedchem.3c00849 | ||
| CHEMBL5421394 | 196325 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | Inhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assayInhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assay |
ChEMBL | 526 | 10 | 4 | 9 | 3.8 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)CCNC(=O)OC(C)(C)C)c2O)c(=O)c1=O)c1ccc(C)o1 | 10.1021/acs.jmedchem.3c00849 | ||
| 163322283 | 190918 | None | 3 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.4 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2cnccc12 | 10.1016/j.ejmech.2023.115240 | ||
| CHEMBL5183834 | 190918 | None | 3 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.4 | C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2cnccc12 | 10.1016/j.ejmech.2023.115240 | ||
| 56839294 | 123073 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | 1 | 2 | Antagonist activity at CXCR2 (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 analysisAntagonist activity at CXCR2 (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 | 6 | 3 | 5 | 1.8 | CN(Cc1ccc(B(O)O)cc1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609005 | 123073 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | 1 | 2 | Antagonist activity at CXCR2 (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 analysisAntagonist activity at CXCR2 (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 | 6 | 3 | 5 | 1.8 | CN(Cc1ccc(B(O)O)cc1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| 11222420 | 86765 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | 40 | 2 | Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR |
ChEMBL | 368 | 2 | 3 | 7 | 2.5 | O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Cl)N2 | 10.1016/j.bmcl.2007.05.011 | ||
| CHEMBL231924 | 86765 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | 40 | 2 | Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR |
ChEMBL | 368 | 2 | 3 | 7 | 2.5 | O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Cl)N2 | 10.1016/j.bmcl.2007.05.011 | ||
| 66856548 | 104689 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 305 | 4 | 2 | 5 | 2.0 | OCc1cc2nc(CCc3cccc(F)c3F)cc(O)n2n1 | 10.1016/j.bmcl.2013.11.074 | ||
| CHEMBL3104899 | 104689 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 305 | 4 | 2 | 5 | 2.0 | OCc1cc2nc(CCc3cccc(F)c3F)cc(O)n2n1 | 10.1016/j.bmcl.2013.11.074 | ||
| 72947877 | 104692 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 431 | 6 | 1 | 8 | 4.8 | Oc1cc(CSc2nc(-c3ccccc3)cs2)nc2nc(Cc3ccccc3)nn12 | 10.1016/j.bmcl.2013.11.074 | ||
| CHEMBL3104904 | 104692 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 431 | 6 | 1 | 8 | 4.8 | Oc1cc(CSc2nc(-c3ccccc3)cs2)nc2nc(Cc3ccccc3)nn12 | 10.1016/j.bmcl.2013.11.074 | ||
| 72948068 | 104694 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 408 | 7 | 1 | 8 | 3.7 | COc1ccc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(OC)c1 | 10.1016/j.bmcl.2013.11.074 | ||
| CHEMBL3104906 | 104694 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method |
ChEMBL | 408 | 7 | 1 | 8 | 3.7 | COc1ccc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(OC)c1 | 10.1016/j.bmcl.2013.11.074 | ||
| 170901566 | 197174 | None | 1 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -12 | 2 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 310 | 9 | 3 | 7 | 2.2 | CCCCCCSc1nc(N[C@H](C)CO)c2nn[nH]c2n1 | 10.1016/j.ejmech.2023.115240 | ||
| CHEMBL5440411 | 197174 | None | 1 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -12 | 2 | Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assayAntagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay |
ChEMBL | 310 | 9 | 3 | 7 | 2.2 | CCCCCCSc1nc(N[C@H](C)CO)c2nn[nH]c2n1 | 10.1016/j.ejmech.2023.115240 | ||
Showing 1 to 50 of 640 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | 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 (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | 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
| |
| 8497 | 2737 | None | 41 | Human | Binding | pIC50 | = | 10.3 | 10.3 | 39 | 2 | Binding affinity to CXCR2Binding affinity to CXCR2 |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/jm300682j | ||
| 9865554 | 2737 | None | 41 | Human | Binding | pIC50 | = | 10.3 | 10.3 | 39 | 2 | Binding affinity to CXCR2Binding affinity to CXCR2 |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/jm300682j | ||
| CHEMBL216981 | 2737 | None | 41 | Human | Binding | pIC50 | = | 10.3 | 10.3 | 39 | 2 | Binding affinity to CXCR2Binding affinity to CXCR2 |
ChEMBL | 397 | 7 | 3 | 7 | 2.9 | CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C | 10.1021/jm300682j | ||
| 11372270 | 67525 | None | 26 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1021/acs.jmedchem.8b00875 | ||
| 11372270.0 | 67525 | None | 26 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1021/acs.jmedchem.8b00875 | ||
| CHEMBL189475 | 67525 | None | 26 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1021/acs.jmedchem.8b00875 | ||
| CHEMBL4442431 | 67525 | None | 26 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin) |
ChEMBL | 375 | 5 | 1 | 6 | 1.1 | C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 | 10.1021/acs.jmedchem.8b00875 | ||
| 88545431 | 171496 | None | 0 | Mouse | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2-mediated chemotaxis in mouse BAF3 cellsInhibition of CXCR2-mediated chemotaxis in mouse BAF3 cells |
ChEMBL | 478 | 7 | 3 | 8 | 3.1 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N3CCN4CCC[C@H]4C3)c2O)c(=O)c1=O)c1ccc(C)o1 | 10.1016/j.ejmech.2019.111853 | ||
| CHEMBL4462143 | 171496 | None | 0 | Mouse | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR2-mediated chemotaxis in mouse BAF3 cellsInhibition of CXCR2-mediated chemotaxis in mouse BAF3 cells |
ChEMBL | 478 | 7 | 3 | 8 | 3.1 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N3CCN4CCC[C@H]4C3)c2O)c(=O)c1=O)c1ccc(C)o1 | 10.1016/j.ejmech.2019.111853 | ||
| 44626319 | 200877 | None | 0 | Human | Binding | pIC50 | = | 9.9 | 9.9 | 81 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 346 | 7 | 3 | 7 | 1.1 | CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O | 10.1016/j.ejmech.2019.111853 | ||
| CHEMBL577075 | 200877 | None | 0 | Human | Binding | pIC50 | = | 9.9 | 9.9 | 81 | 2 | Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin) |
ChEMBL | 346 | 7 | 3 | 7 | 1.1 | CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O | 10.1016/j.ejmech.2019.111853 | ||
| 137633598 | 156522 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 445 | 5 | 3 | 5 | 4.0 | CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)CC(F)(F)F)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4066904 | 156522 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 445 | 5 | 3 | 5 | 4.0 | CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)CC(F)(F)F)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118540892 | 157820 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 377 | 3 | 3 | 5 | 3.1 | CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)C)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4082136 | 157820 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 377 | 3 | 3 | 5 | 3.1 | CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)C)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118554832 | 159325 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 432 | 4 | 3 | 5 | 3.5 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4098864 | 159325 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 432 | 4 | 3 | 5 | 3.5 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 72548703 | 161661 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysis |
ChEMBL | 583 | 8 | 3 | 6 | 5.8 | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 | 10.1016/j.bmcl.2018.03.093 | ||
| CHEMBL4128926 | 161661 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Displacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysis |
ChEMBL | 583 | 8 | 3 | 6 | 5.8 | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 | 10.1016/j.bmcl.2018.03.093 | ||
| 129316069 | 155944 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 436 | 6 | 4 | 5 | 3.4 | CC(C)(CCO)S(=O)(=O)c1c(Cl)ccc(NC(=O)N[C@@H]2CCC=C2Cl)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4060139 | 155944 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 436 | 6 | 4 | 5 | 3.4 | CC(C)(CCO)S(=O)(=O)c1c(Cl)ccc(NC(=O)N[C@@H]2CCC=C2Cl)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118554743 | 156125 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 428 | 5 | 3 | 5 | 3.5 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(C)C2COC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4062361 | 156125 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 428 | 5 | 3 | 5 | 3.5 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(C)C2COC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118540867 | 157001 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 414 | 4 | 4 | 5 | 3.0 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CC[C@@H](O)C2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4072270 | 157001 | None | 0 | Human | Binding | pIC50 | = | 9.6 | 9.6 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 414 | 4 | 4 | 5 | 3.0 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CC[C@@H](O)C2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 129316028 | 157406 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 442 | 5 | 3 | 5 | 4.0 | CCC1(S(=O)(=O)c2c(Cl)ccc(NC(=O)N[C@@H]3CCC=C3C)c2O)CCOCC1 | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4077201 | 157406 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 442 | 5 | 3 | 5 | 4.0 | CCC1(S(=O)(=O)c2c(Cl)ccc(NC(=O)N[C@@H]3CCC=C3C)c2O)CCOCC1 | 10.1021/acs.jmedchem.7b01854 | ||
| 58180205 | 140891 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 446 | 4 | 3 | 4 | 5.2 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| CHEMBL3818853 | 140891 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 446 | 4 | 3 | 4 | 5.2 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| 58180198 | 140903 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 432 | 4 | 3 | 4 | 4.8 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| CHEMBL3818984 | 140903 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 432 | 4 | 3 | 4 | 4.8 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| 58180199 | 140937 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 460 | 4 | 3 | 4 | 5.6 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| CHEMBL3819480 | 140937 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 460 | 4 | 3 | 4 | 5.6 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCCC2)c1O)Nc1cccc(F)c1Cl | 10.1021/acsmedchemlett.5b00489 | ||
| 127049431 | 140817 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 420 | 4 | 3 | 4 | 4.7 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC(=O)Nc2cccc(F)c2Cl)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL3817901 | 140817 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 420 | 4 | 3 | 4 | 4.7 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC(=O)Nc2cccc(F)c2Cl)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 123190913 | 156516 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 372 | 4 | 3 | 4 | 3.5 | CC1=CCCC1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)C)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4066818 | 156516 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 372 | 4 | 3 | 4 | 3.5 | CC1=CCCC1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)C)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 129316018 | 156832 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 467 | 5 | 3 | 5 | 4.1 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCN(C3CCC3)CC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4070506 | 156832 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 467 | 5 | 3 | 5 | 4.1 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCN(C3CCC3)CC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118540730 | 158215 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 394 | 4 | 3 | 4 | 3.7 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(F)F)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4086957 | 158215 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 394 | 4 | 3 | 4 | 3.7 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(F)F)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 127052173 | 140870 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 543 | 4 | 3 | 5 | 5.9 | CN1CCC2(CCC(S(=O)(=O)c3c(Cl)ccc(NC(=O)Nc4cccc(F)c4Cl)c3O)CC2)CC1 | 10.1021/acsmedchemlett.5b00489 | ||
| CHEMBL3818581 | 140870 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 543 | 4 | 3 | 5 | 5.9 | CN1CCC2(CCC(S(=O)(=O)c3c(Cl)ccc(NC(=O)Nc4cccc(F)c4Cl)c3O)CC2)CC1 | 10.1021/acsmedchemlett.5b00489 | ||
| 127051854 | 140911 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 487 | 4 | 3 | 5 | 4.4 | CN1CC2(CC(S(=O)(=O)c3c(Cl)ccc(NC(=O)Nc4cccc(F)c4Cl)c3O)C2)C1 | 10.1021/acsmedchemlett.5b00489 | ||
| CHEMBL3819163 | 140911 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation |
ChEMBL | 487 | 4 | 3 | 5 | 4.4 | CN1CC2(CC(S(=O)(=O)c3c(Cl)ccc(NC(=O)Nc4cccc(F)c4Cl)c3O)C2)C1 | 10.1021/acsmedchemlett.5b00489 | ||
| 118554794 | 156493 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 428 | 4 | 3 | 5 | 3.6 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(C)CCOCC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4066510 | 156493 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 428 | 4 | 3 | 5 | 3.6 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(C)CCOCC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
| 118554809 | 157808 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 452 | 4 | 3 | 5 | 3.7 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O)N[C@@H]1CCC=C1Cl | 10.1021/acs.jmedchem.7b01854 | ||
| CHEMBL4082031 | 157808 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 452 | 4 | 3 | 5 | 3.7 | O=C(Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O)N[C@@H]1CCC=C1Cl | 10.1021/acs.jmedchem.7b01854 | ||
| 118554742 | 158343 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay |
ChEMBL | 456 | 5 | 3 | 5 | 4.3 | CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(C)C2CCOCC2)c1O | 10.1021/acs.jmedchem.7b01854 | ||
Showing 1 to 50 of 2,080 entries