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
| |
| 162647583 | 180005 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -25 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | ||
| CHEMBL4745933 | 180005 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -25 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | ||
| 162652088 | 180367 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -707 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 359 | 4 | 3 | 6 | 1.9 | CCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4750465 | 180367 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -707 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 359 | 4 | 3 | 6 | 1.9 | CCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| 162675855 | 183417 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -45 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 425 | 4 | 3 | 6 | 3.0 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(F)cc3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4797191 | 183417 | None | 0 | Human | Functional | pIC50 | = | 4 | 4.0 | -45 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 425 | 4 | 3 | 6 | 3.0 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(F)cc3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| 122187259 | 123075 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -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 analysisAntagonist 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 | 6 | 4 | 6 | 1.2 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2cccc(B(O)O)c2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609008 | 123075 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -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 analysisAntagonist 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 | 6 | 4 | 6 | 1.2 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2cccc(B(O)O)c2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 56839294 | 123073 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -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 analysisAntagonist 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 | 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 | = | 5.9 | 5.9 | -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 analysisAntagonist 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 | 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 | ||
| 162673727 | 183089 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -218 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 373 | 5 | 3 | 6 | 2.3 | CCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4793352 | 183089 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -218 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 373 | 5 | 3 | 6 | 2.3 | CCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| 8497 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.8 | 6.8 | -5 | 4 | Antagonist activity in CXCR1 (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 CXCR1 (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 | = | 6.8 | 6.8 | -5 | 4 | Antagonist activity in CXCR1 (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 CXCR1 (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 | = | 6.8 | 6.8 | -5 | 4 | Antagonist activity in CXCR1 (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 CXCR1 (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 | ||
| 122187257 | 123074 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -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 analysisAntagonist 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 | 6 | 3 | 6 | 1.2 | CN(Cc1ccc(B(O)O)cn1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609006 | 123074 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -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 analysisAntagonist 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 | 6 | 3 | 6 | 1.2 | CN(Cc1ccc(B(O)O)cn1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| 122187261 | 123077 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 analysisAntagonist 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 | 6 | 4 | 6 | 1.2 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2ccc(B(O)O)cc2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609010 | 123077 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 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 analysisAntagonist 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 | 6 | 4 | 6 | 1.2 | O=C(Nc1ccc(F)cc1)c1cnc(NCc2ccc(B(O)O)cc2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 122187262 | 123079 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -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 analysisAntagonist 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 | 6 | 3 | 7 | 0.6 | CN(Cc1ccc(B(O)O)cn1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609012 | 123079 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -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 analysisAntagonist 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 | 6 | 3 | 7 | 0.6 | CN(Cc1ccc(B(O)O)cn1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| 8497 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP based fluorescence assayAntagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP 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 | 10.1016/j.ejmech.2020.112537 | ||
| 9865554 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP based fluorescence assayAntagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP 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 | 10.1016/j.ejmech.2020.112537 | ||
| CHEMBL216981 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP based fluorescence assayAntagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP 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 | 10.1016/j.ejmech.2020.112537 | ||
| 8497 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM based fluorescence assayAntagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM 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 | 10.1016/j.ejmech.2019.111914 | ||
| 9865554 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM based fluorescence assayAntagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM 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 | 10.1016/j.ejmech.2019.111914 | ||
| CHEMBL216981 | 2737 | None | 41 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -5 | 4 | Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM based fluorescence assayAntagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM 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 | 10.1016/j.ejmech.2019.111914 | ||
| 162648477 | 180068 | None | 0 | Human | Functional | pIC50 | = | 4.7 | 4.7 | -707 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 373 | 5 | 3 | 6 | 2.3 | CCC[C@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4746698 | 180068 | None | 0 | Human | Functional | pIC50 | = | 4.7 | 4.7 | -707 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 373 | 5 | 3 | 6 | 2.3 | CCC[C@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O | 10.1021/acsmedchemlett.1c00113 | ||
| 122187269 | 123085 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | 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 analysisAntagonist 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 | 8 | 3 | 8 | 1.5 | O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609019 | 123085 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | 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 analysisAntagonist 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 | 8 | 3 | 8 | 1.5 | O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 162652658 | 180545 | None | 0 | Human | Functional | pIC50 | = | 4.7 | 4.7 | -407 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 441 | 4 | 3 | 6 | 3.5 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3Cl)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4752486 | 180545 | None | 0 | Human | Functional | pIC50 | = | 4.7 | 4.7 | -407 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 441 | 4 | 3 | 6 | 3.5 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3Cl)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| 162657065 | 181007 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | -1548 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 522 | 7 | 4 | 8 | 3.4 | CC(C)(C)OC(=O)NCCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| CHEMBL4757674 | 181007 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | -1548 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 522 | 7 | 4 | 8 | 3.4 | CC(C)(C)OC(=O)NCCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
| 122187260 | 123076 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | 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 analysisAntagonist 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 | 6 | 3 | 6 | 1.2 | CN(Cc1cccc(B(O)O)c1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609009 | 123076 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | 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 analysisAntagonist 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 | 6 | 3 | 6 | 1.2 | CN(Cc1cccc(B(O)O)c1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 | 10.1016/j.bmcl.2015.07.090 | ||
| 155531736 | 171777 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -60 | 2 | Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 395 | 5 | 3 | 6 | 2.6 | O=C(c1cccc(Nc2c(NC3C[C@@H]4CC[C@H]3C4)c(=O)c2=O)c1O)N1CCCC1 | 10.1016/j.ejmech.2019.111853 | ||
| CHEMBL4466314 | 171777 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -60 | 2 | Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay |
ChEMBL | 395 | 5 | 3 | 6 | 2.6 | O=C(c1cccc(Nc2c(NC3C[C@@H]4CC[C@H]3C4)c(=O)c2=O)c1O)N1CCCC1 | 10.1016/j.ejmech.2019.111853 | ||
| 122187266 | 123083 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | 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 analysisAntagonist 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 | 8 | 3 | 7 | 2.3 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609016 | 123083 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | 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 analysisAntagonist 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 | 8 | 3 | 7 | 2.3 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 46897163 | 119147 | None | 5 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 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 analysisAntagonist 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 | 7 | 3 | 6 | 3.3 | O=C(Nc1ccc(F)cc1)c1ccc(SCc2cc(OC(F)(F)F)ccc2B(O)O)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3426944 | 119147 | None | 5 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 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 analysisAntagonist 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 | 7 | 3 | 6 | 3.3 | O=C(Nc1ccc(F)cc1)c1ccc(SCc2cc(OC(F)(F)F)ccc2B(O)O)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 122187263 | 123080 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | -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 analysisAntagonist 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 | 8 | 3 | 6 | 2.8 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| CHEMBL3609013 | 123080 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | -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 analysisAntagonist 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 | 8 | 3 | 6 | 2.8 | O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 | 10.1016/j.bmcl.2015.07.090 | ||
| 10112327 | 126297 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophilsInhibition of interleukin-8 induced elastase release from human neutrophils |
ChEMBL | 411 | 7 | 0 | 5 | 4.7 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(Cl)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| CHEMBL365008 | 126297 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophilsInhibition of interleukin-8 induced elastase release from human neutrophils |
ChEMBL | 411 | 7 | 0 | 5 | 4.7 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(Cl)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| 9843640 | 65681 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophilsInhibition of interleukin-8 induced elastase release from human neutrophils |
ChEMBL | 395 | 7 | 0 | 5 | 4.2 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(F)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| CHEMBL183425 | 65681 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | Inhibition of interleukin-8 induced elastase release from human neutrophilsInhibition of interleukin-8 induced elastase release from human neutrophils |
ChEMBL | 395 | 7 | 0 | 5 | 4.2 | CN1CCN(CCCOc2ccc(-c3cc(-c4ccc(F)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| 162656425 | 180985 | None | 0 | Human | Functional | pIC50 | = | 4.4 | 4.4 | -41 | 2 | Antagonist activity in CXCR1 (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 CXCR1 (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 | 441 | 4 | 3 | 6 | 3.5 | CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(Cl)cc3)N2)c1O | 10.1021/acsmedchemlett.1c00113 | ||
Showing 1 to 50 of 100 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
| |
| 11372270 | 67525 | None | 26 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | Inhibition of CXCR1 (unknown origin)Inhibition of CXCR1 (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 CXCR1 (unknown origin)Inhibition of CXCR1 (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 CXCR1 (unknown origin)Inhibition of CXCR1 (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 CXCR1 (unknown origin)Inhibition of CXCR1 (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 | ||
| 8498 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Binding affinity to CXCR1Binding affinity to CXCR1 |
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 | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Binding affinity to CXCR1Binding affinity to CXCR1 |
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 | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Binding affinity to CXCR1Binding affinity to CXCR1 |
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 | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Binding affinity to CXCR1Binding affinity to CXCR1 |
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 | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Binding affinity to CXCR1Binding affinity to CXCR1 |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1021/jm300682j | ||
| 8498 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of 125I-IL-8 from CXCR1 (unknown origin)Displacement of 125I-IL-8 from CXCR1 (unknown origin) |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1016/j.ejmech.2023.115175 | ||
| 9838712 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of 125I-IL-8 from CXCR1 (unknown origin)Displacement of 125I-IL-8 from CXCR1 (unknown origin) |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1016/j.ejmech.2023.115175 | ||
| 9838712.0 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of 125I-IL-8 from CXCR1 (unknown origin)Displacement of 125I-IL-8 from CXCR1 (unknown origin) |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1016/j.ejmech.2023.115175 | ||
| CHEMBL191413 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of 125I-IL-8 from CXCR1 (unknown origin)Displacement of 125I-IL-8 from CXCR1 (unknown origin) |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1016/j.ejmech.2023.115175 | ||
| DB12614 | 3315 | None | 44 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Displacement of 125I-IL-8 from CXCR1 (unknown origin)Displacement of 125I-IL-8 from CXCR1 (unknown origin) |
ChEMBL | 283 | 5 | 1 | 3 | 2.1 | CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C | 10.1016/j.ejmech.2023.115175 | ||
| 44419482 | 83267 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 505 | 4 | 3 | 5 | 3.8 | CN(C)S(=O)(=O)c1c(C(F)(F)F)ccc(N/C(=N/C#N)Nc2ccccc2Br)c1O | 10.1016/j.bmcl.2006.08.042 | ||
| CHEMBL218665 | 83267 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 505 | 4 | 3 | 5 | 3.8 | CN(C)S(=O)(=O)c1c(C(F)(F)F)ccc(N/C(=N/C#N)Nc2ccccc2Br)c1O | 10.1016/j.bmcl.2006.08.042 | ||
| 3793 | 205667 | None | 50 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 1 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 704 | 11 | 0 | 12 | 5.6 | CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O | 10.1021/jm301749y | ||
| 45039617 | 205667 | None | 50 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 1 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 704 | 11 | 0 | 12 | 5.6 | CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O | 10.1021/jm301749y | ||
| CHEMBL64391 | 205667 | None | 50 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 1 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 704 | 11 | 0 | 12 | 5.6 | CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O | 10.1021/jm301749y | ||
| 44446593 | 94863 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 417 | 7 | 3 | 7 | 3.2 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1cc(Cl)co1 | 10.1016/j.bmcl.2008.01.024 | ||
| CHEMBL253497 | 94863 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 417 | 7 | 3 | 7 | 3.2 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1cc(Cl)co1 | 10.1016/j.bmcl.2008.01.024 | ||
| 11329244 | 71140 | None | 6 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of C-X-C chemokine receptor type 1Inhibition of C-X-C chemokine receptor type 1 |
ChEMBL | 486 | 7 | 2 | 5 | 5.4 | CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C | 10.1021/jm049530m | ||
| CHEMBL195433 | 71140 | None | 6 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of C-X-C chemokine receptor type 1Inhibition of C-X-C chemokine receptor type 1 |
ChEMBL | 486 | 7 | 2 | 5 | 5.4 | CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C | 10.1021/jm049530m | ||
| 11272103 | 124442 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of C-X-C chemokine receptor type 1Inhibition of C-X-C chemokine receptor type 1 |
ChEMBL | 505 | 7 | 2 | 6 | 4.7 | Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 | 10.1021/jm049530m | ||
| CHEMBL363840 | 124442 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of C-X-C chemokine receptor type 1Inhibition of C-X-C chemokine receptor type 1 |
ChEMBL | 505 | 7 | 2 | 6 | 4.7 | Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 | 10.1021/jm049530m | ||
| 2812 | 4781 | None | 63 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 34 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 344 | 4 | 0 | 2 | 5.4 | Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 | 10.1021/jm301749y | ||
| CHEMBL104 | 4781 | None | 63 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 34 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 344 | 4 | 0 | 2 | 5.4 | Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 | 10.1021/jm301749y | ||
| 44446605 | 94893 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 461 | 7 | 3 | 7 | 3.4 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1occc1Br | 10.1016/j.bmcl.2008.01.024 | ||
| CHEMBL253707 | 94893 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 461 | 7 | 3 | 7 | 3.4 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1occc1Br | 10.1016/j.bmcl.2008.01.024 | ||
| 44419479 | 84337 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 578 | 8 | 4 | 7 | 4.0 | CCC(CC)(NS(=O)(=O)c1c(C)ccc(N/C(=N/C#N)Nc2ccccc2Br)c1O)N1CCOCC1 | 10.1016/j.bmcl.2006.08.042 | ||
| CHEMBL221481 | 84337 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 578 | 8 | 4 | 7 | 4.0 | CCC(CC)(NS(=O)(=O)c1c(C)ccc(N/C(=N/C#N)Nc2ccccc2Br)c1O)N1CCOCC1 | 10.1016/j.bmcl.2006.08.042 | ||
| 44446647 | 155194 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 399 | 7 | 3 | 7 | 3.1 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccsc1 | 10.1016/j.bmcl.2008.01.024 | ||
| CHEMBL401940 | 155194 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 399 | 7 | 3 | 7 | 3.1 | CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccsc1 | 10.1016/j.bmcl.2008.01.024 | ||
| 10157580 | 66331 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligandInhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand |
ChEMBL | 396 | 7 | 0 | 6 | 3.6 | CN1CCN(CCCOc2ccc(-c3nc(-c4ccc(F)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| CHEMBL184882 | 66331 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligandInhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand |
ChEMBL | 396 | 7 | 0 | 6 | 3.6 | CN1CCN(CCCOc2ccc(-c3nc(-c4ccc(F)cc4)no3)cc2)CC1 | 10.1016/j.bmcl.2004.05.080 | ||
| 44393540 | 166185 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligandInhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand |
ChEMBL | 294 | 5 | 0 | 4 | 3.9 | CN(C)COc1ccc(-c2cc(-c3ccccc3)on2)cc1 | 10.1016/j.bmcl.2004.05.080 | ||
| CHEMBL425882 | 166185 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligandInhibitory concentration against interleukin-8 receptor of human neutrophils by using [125I]IL-8 (0.125 nM) as radioligand |
ChEMBL | 294 | 5 | 0 | 4 | 3.9 | CN(C)COc1ccc(-c2cc(-c3ccccc3)on2)cc1 | 10.1016/j.bmcl.2004.05.080 | ||
| 71526067 | 143987 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences).In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences). |
ChEMBL | 539 | 8 | 3 | 10 | 3.5 | COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(NC(c3ccc(C)o3)C3CCCS3)c(=O)c2=O)c1O | nan | ||
| CHEMBL3901913 | 143987 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences).In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences). |
ChEMBL | 539 | 8 | 3 | 10 | 3.5 | COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(NC(c3ccc(C)o3)C3CCCS3)c(=O)c2=O)c1O | nan | ||
| 2812 | 4781 | None | 63 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 34 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 344 | 4 | 0 | 2 | 5.4 | Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 | 10.1021/jm301749y | ||
| CHEMBL104 | 4781 | None | 63 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 34 | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 344 | 4 | 0 | 2 | 5.4 | Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 | 10.1021/jm301749y | ||
| 44419476 | 136476 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 562 | 8 | 4 | 7 | 4.6 | CCC(CC)(NS(=O)(=O)c1c(Cl)ccc(N/C(=N/C#N)Nc2ccccc2C)c1O)N1C[C@H](C)O[C@H](C)C1 | 10.1016/j.bmcl.2006.08.042 | ||
| CHEMBL373522 | 136476 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]IL8 from CXCR1 expressed in CHO cellsDisplacement of [125I]IL8 from CXCR1 expressed in CHO cells |
ChEMBL | 562 | 8 | 4 | 7 | 4.6 | CCC(CC)(NS(=O)(=O)c1c(Cl)ccc(N/C(=N/C#N)Nc2ccccc2C)c1O)N1C[C@H](C)O[C@H](C)C1 | 10.1016/j.bmcl.2006.08.042 | ||
| 71526159 | 145487 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences).In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences). |
ChEMBL | 525 | 8 | 3 | 9 | 3.6 | Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2CCCS2)o1 | nan | ||
| CHEMBL3913959 | 145487 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences).In Vitro Affinity Assay: â¿¿PathHunter HEK293-CXCR2â¿ or â¿¿U2OS hCXCR1 β-arrestinâ¿ cells (DiscoveRx Corporation) were seeded overnight at 10 000 cells/well (384-well format) in 20 μl of Opti MEM I medium. A preincubation with the antagonist or the vehicle for 30 min at 37° C. and 5% CO2 was followed by 60 minutes of stimulation with CXCL8 at 37° C. and 5% CO2. The cells were then placed at ambient temperature for 30 minutes. The PathHunter detection reagent (DiscoveRx Corporation) was added. After incubation for 60 min at ambient temperature, the β-galactosidase induced by the luminescence during the β-arrestin-CXCR2 interaction was measured for 0.3 s in an Envision 2102 Multilabel Reader (PerkinElmer Life and Analytical Sciences). |
ChEMBL | 525 | 8 | 3 | 9 | 3.6 | Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2CCCS2)o1 | nan | ||
| 16098488 | 138050 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cellsDisplacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells |
ChEMBL | 425 | 6 | 3 | 7 | 3.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C(C)(C)C)o1 | 10.1021/jm0609622 | ||
| CHEMBL376414 | 138050 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cellsDisplacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells |
ChEMBL | 425 | 6 | 3 | 7 | 3.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C(C)(C)C)o1 | 10.1021/jm0609622 | ||
| 44446621 | 155575 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 433 | 7 | 3 | 7 | 3.7 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(Cl)s1 | 10.1016/j.bmcl.2008.01.024 | ||
| CHEMBL404060 | 155575 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of CXCR1Inhibition of CXCR1 |
ChEMBL | 433 | 7 | 3 | 7 | 3.7 | CCC(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(Cl)s1 | 10.1016/j.bmcl.2008.01.024 | ||
| 21184843 | 97241 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibition of binding of IL-8 to membranes of cloned CXC chemokine receptor 1 expressed in CHO Cells using [125I]IL-8 radioligandInhibition of binding of IL-8 to membranes of cloned CXC chemokine receptor 1 expressed in CHO Cells using [125I]IL-8 radioligand |
ChEMBL | 365 | 2 | 3 | 3 | 4.3 | N#Cc1c(Cl)ccc(NC(=O)Nc2ccccc2Br)c1O | 10.1021/jm034248l | ||
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