Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL217378 c5ar1_human Human No 8.9 EC50 = 1.3 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL217378 c5ar1_human Human No 7.9 EC50 = 12.3 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL265884 c5ar1_human Human No 5.9 EC50 = 1200 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL471412 c5ar1_human Human No 6.9 EC50 = 123.0 nM Funct
Antagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS bindingAntagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS binding
476 8 1 4 5.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL427936 c5ar1_human Human No 4.8 EC50 = 15800 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL262653 c5ar1_human Human No 4.7 EC50 = 19500 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL269480 c5ar1_human Human No 5.7 EC50 = 2000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL429535 c5ar1_human Human No 5.7 EC50 = 2100 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL412680 c5ar1_human Human No 4.7 EC50 = 22000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL268322 c5ar1_human Human No 5.6 EC50 = 2300 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL414361 c5ar1_human Human No 5.6 EC50 = 2500 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL408796 c5ar1_human Human No 4.6 EC50 = 27700 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL408796 c5ar1_human Human No 6.5 EC50 = 300 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL265884 c5ar1_human Human No 4.5 EC50 = 32000 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL406011 c5ar1_human Human Yes 4.4 EC50 = 37000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL406011 c5ar1_human Human Yes 5.4 EC50 = 4000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL438728 c5ar1_human Human No 5.4 EC50 = 4000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL412680 c5ar1_human Human No 4.4 EC50 = 42000 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL414361 c5ar1_human Human No 4.3 EC50 = 46500 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL386427 c5ar1_human Human No 4.3 EC50 = 48000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL269480 c5ar1_human Human No 4.3 EC50 = 49600 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL435318 c5ar1_human Human No 5.3 EC50 = 5000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL405966 c5ar1_human Human No 4.3 EC50 = 50000 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL406011 c5ar1_human Human Yes 4.3 EC50 = 50000 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL412249 c5ar1_human Human No 5.3 EC50 = 5600 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL429535 c5ar1_human Human No 4.2 EC50 = 57700 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL441393 c5ar1_human Human No 4.2 EC50 = 67700 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL374912 c5ar1_human Human No 4.2 EC50 = 70000 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL435318 c5ar1_human Human No 4.1 EC50 = 80000 nM Funct
Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)
None None None None
CHEMBL441393 c5ar1_human Human No 6.1 EC50 = 900 nM Funct
Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)
None None None None
CHEMBL3646938 c5ar1_human Human No 9.3 IC50 = 0.5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
498 5 0 5 6.8 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646964 c5ar1_human Human No 9.3 IC50 = 0.5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
540 5 1 8 5.1 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human HL60 cells assessed as inhibition of recombinant human C5a-induced oxidative burst after 30 mins by fluorescence assayAntagonist activity at C5aR1 in human HL60 cells assessed as inhibition of recombinant human C5a-induced oxidative burst after 30 mins by fluorescence assay
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced cell degranulation preincubated for 30 mins followed by C5a-induction and measured after 30 mins by beta-glucuronidase activity-based assayAntagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced cell degranulation preincubated for 30 mins followed by C5a-induction and measured after 30 mins by beta-glucuronidase activity-based assay
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced chemotaxis preincubated for 30 mins followed by C5a-induction and measured after 1 hr by fluorometerAntagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced chemotaxis preincubated for 30 mins followed by C5a-induction and measured after 1 hr by fluorometer
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced intracellular calcium mobilization preincubated for 1 hr followed by human C5a-induction by Fluo-3 dye-based FLIPR assayAntagonist activity at C5aR1 in human U937 cells assessed as inhibition of recombinant human C5a-induced intracellular calcium mobilization preincubated for 1 hr followed by human C5a-induction by Fluo-3 dye-based FLIPR assay
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human blood granulocytes assessed as inhibition of recombinant human C5a-induced CD11b expression on granulocytes preincubated for 15 mins followed by C5a-induction and measured after 2 to 5 mins by flow cytometric analysisAntagonist activity at C5aR1 in human blood granulocytes assessed as inhibition of recombinant human C5a-induced CD11b expression on granulocytes preincubated for 15 mins followed by C5a-induction and measured after 2 to 5 mins by flow cytometric analysis
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at C5aR1 in human neutrophils assessed as inhibition of recombinant human C5a-induced chemotaxis preincubated for 30 mins followed by C5a-induction and measured after 1 hr by fluorometerAntagonist activity at C5aR1 in human neutrophils assessed as inhibition of recombinant human C5a-induced chemotaxis preincubated for 30 mins followed by C5a-induction and measured after 1 hr by fluorometer
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL4245250 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at recombinant human C5aR1 expressed in Sf9 insect cell membranes co-expressing G-alphai2,G-beta1 and G-gamma2 assessed as inhibition of recombinant human C5a-induced [35S]GTPgammaS binding after 60 mins by liquid scintillation spectrometryAntagonist activity at recombinant human C5aR1 expressed in Sf9 insect cell membranes co-expressing G-alphai2,G-beta1 and G-gamma2 assessed as inhibition of recombinant human C5a-induced [35S]GTPgammaS binding after 60 mins by liquid scintillation spectrometry
559 10 0 7 7.7 CCCCn1c(-c2ccccc2)nc(-c2ccccc2)c1N(Cc1ccc2c(c1)OCO2)Cc1ccc2c(c1)OCO2
CHEMBL3646934 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
538 5 1 6 6.5 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@H]1C
CHEMBL3646944 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
538 5 1 6 6.6 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646945 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
566 5 1 7 5.8 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C4(C)COC4)ccc2C)CC3)[C@H](C)C1
CHEMBL3646951 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
530 4 1 6 6.2 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(Cl)ccc2C)CC3)[C@H](C)C1
CHEMBL3646952 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
564 4 1 6 6.5 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(F)(F)F)ccc2C)CC3)[C@H](C)C1
CHEMBL3646953 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
552 5 1 6 6.9 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646956 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
552 6 1 6 7.0 CCO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646957 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
508 4 1 5 7.0 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CCCC[C@H]3C)c2C1
CHEMBL3646963 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
526 5 1 8 4.8 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C4CC4)nn2C)CC3)[C@H](C)C1
CHEMBL3647001 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
551 6 2 6 4.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(CC(N)=O)C[C@H]3C)c2C1
CHEMBL3647006 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
584 5 1 8 5.8 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C(F)F)nn2C)CC3)CC1(C)C
CHEMBL3647009 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
560 5 1 8 5.5 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)[C@H](C)C1
CHEMBL3647012 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
558 5 1 8 5.2 CO[C@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(F)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL3647014 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
568 5 1 8 5.3 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(F)c(C(F)F)nn2C)CC3)CC1(C)C
CHEMBL3647018 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
509 5 1 6 5.4 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CC(N(C)C)C3)c2C1
CHEMBL3647021 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
480 4 1 5 6.2 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CCC3C)c2C1
CHEMBL3647028 c5ar1_human Human No 9.0 IC50 = 1 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
558 4 1 8 5.1 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3CC[C@@H]4OC[C@]4(C)C3)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL486749 c5ar1_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
455 7 0 3 5.9 CC(C)Cc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL3646905 c5ar1_human Human No 8.0 IC50 = 10 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
430 5 1 5 4.8 Cc1ccccc1N1CCc2nc(-c3c(C)cccc3C)nc(N(C)CC(C)(C)O)c2C1
CHEMBL3646908 c5ar1_human Human No 8.0 IC50 = 10 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 5 1 5 6.9 CO[C@@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646915 c5ar1_human Human No 8.0 IC50 = 10 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
467 4 2 5 5.1 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CC(O)C3)c2C1
CHEMBL259769 c5ar1_human Human No 7.0 IC50 = 100 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
464 7 0 3 7.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL469727 c5ar1_human Human No 7.0 IC50 = 100 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
500 11 2 7 3.5 COCc1ccoc1C(=O)N(c1ccc(OC)cc1OC)C(C(=O)NC[C@@H](C)O)c1ccccc1F
CHEMBL513757 c5ar1_human Human No 6.0 IC50 = 1000 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
493 10 1 5 4.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC(C)CN(C)C)c2ccccc2F)c(OC)c1
CHEMBL173394 c5ar1_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
359 7 2 2 4.7 C/N=C(/N)Nc1ccc(OCCCc2ccccc2)c(-c2ccccc2)c1
CHEMBL173442 c5ar1_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
351 6 2 2 5.1 C/N=C(/N)Nc1ccc(OCCC2CCCCC2)c(-c2ccccc2)c1
CHEMBL486959 c5ar1_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
490 10 0 3 6.1 COc1ccc(CCCN2CCC(N(CCc3ccc(Cl)cc3)C(=O)c3ccccc3)CC2)cc1
CHEMBL528767 c5ar1_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
429 6 0 4 4.7 COc1cccc(C(=O)N(CCc2ccc(Cl)cc2)C2CCC3(CC2)OCCO3)c1
CHEMBL69007 c5ar1_human Human No 6.0 IC50 = 1000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
497 9 4 5 1.9 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCN(c3ccccc3)CC2)C1=O
CHEMBL291792 c5ar1_human Human No 5.0 IC50 = 10000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CNC1=O
CHEMBL385012 c5ar1_human Human No 4.0 IC50 = 100000 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL41547 c5ar1_human Human Yes 7.0 IC50 = 104 nM Bind
Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells
None None None None
CHEMBL407439 c5ar1_human Human No 7.0 IC50 = 107 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CCCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(C)=O)CCCNC1=O
CHEMBL3646989 c5ar1_human Human No 8.0 IC50 = 11 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
410 5 0 2 6.9 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CCN(c1cc(C3CC3)ccc1C)C2
CHEMBL411265 c5ar1_human Human No 7.0 IC50 = 110 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
472 6 0 4 7.5 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3c(Cl)cccc3OC)cc(OC)c21
CHEMBL471009 c5ar1_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
450 5 0 4 5.3 O=C(c1cccc2cnccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL258658 c5ar1_human Human No 6.0 IC50 = 1100 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
426 5 0 3 6.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2ccccc2C1
CHEMBL117143 c5ar1_human Human No 5.0 IC50 = 11000 nM Bind
50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL117143 c5ar1_human Human No 5.0 IC50 = 11000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL309154 c5ar1_human Human No 5.0 IC50 = 11000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
566 8 4 4 3.4 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2cccc3ccccc23)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL2371928 c5ar1_human Human No 7.0 IC50 = 111 nM Bind
Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells
None None None CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL3646928 c5ar1_human Human No 7.0 IC50 = 112 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
518 5 1 5 6.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cc(Cl)ccc3CO)nc(N3CCCC(C)(C)C3)c2C1
CHEMBL262178 c5ar1_human Human No 6.9 IC50 = 116 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(C)C)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL115478 c5ar1_human Human No 7.9 IC50 = 12 nM Bind
50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL513344 c5ar1_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
499 7 0 5 5.9 COCC(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3646918 c5ar1_human Human No 7.9 IC50 = 12 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
495 4 2 5 5.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCC[C@H](O)C3)c2C1
CHEMBL3647031 c5ar1_human Human No 7.9 IC50 = 12 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
532 4 1 8 4.7 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3CCOC[C@H]3C)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL481756 c5ar1_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
416 7 2 4 5.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1CO
CHEMBL3350746 c5ar1_human Human No 5.9 IC50 = 1200 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
2082 70 27 26 -1.2 CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O)C(C)C
CHEMBL1790511 c5ar1_human Human No 5.9 IC50 = 1200 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
482 8 3 4 1.9 CC[C@@H](C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL420926 c5ar1_human Human No 5.9 IC50 = 1200 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
468 7 3 4 1.5 CC(C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL3350746 c5ar1_human Human No 5.9 IC50 = 1230.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
2082 70 27 26 -1.2 CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O)C(C)C
CHEMBL518254 c5ar1_human Human No 6.9 IC50 = 125 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
407 5 1 2 5.5 O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1
CHEMBL518254 c5ar1_human Human No 6.9 IC50 = 125 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
407 5 1 2 5.5 O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1
CHEMBL472455 c5ar1_human Human Yes 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
466 8 1 5 4.9 COc1ccc(N(C(=O)c2ccco2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL468430 c5ar1_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
506 7 0 4 5.8 CN(C)CC(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3646907 c5ar1_human Human No 7.9 IC50 = 13 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 5 1 5 6.9 CO[C@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL260476 c5ar1_human Human No 6.9 IC50 = 130 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
436 5 0 3 7.4 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3c(C)cccc3C)cc(OC)c21
CHEMBL3647039 c5ar1_human Human No 6.9 IC50 = 131 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
385 4 0 3 5.8 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CCN(c1c(C)ccnc1C)C2
CHEMBL3646987 c5ar1_human Human No 6.9 IC50 = 132 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
423 3 1 2 6.5 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)cc(C)c2C1=O
CHEMBL3647038 c5ar1_human Human No 7.9 IC50 = 14 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
448 5 0 4 6.4 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CC(C)N(c1c(Cl)c(C3CC3)nn1C)C2
CHEMBL481482 c5ar1_human Human No 6.9 IC50 = 140 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
430 7 1 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(OC)ccc1C
CHEMBL405887 c5ar1_human Human No 5.9 IC50 = 1400 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
460 5 0 3 7.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2ccc(Cl)cc2C1
CHEMBL479391 c5ar1_human Human No 5.9 IC50 = 1400 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
418 6 1 3 6.8 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(F)ccc1C
CHEMBL116851 c5ar1_human Human No 4.9 IC50 = 14000 nM Bind
50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(N)=O
CHEMBL118072 c5ar1_human Human No 4.9 IC50 = 14000 nM Bind
50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL219386 c5ar1_human Human No 6.8 IC50 = 146 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCC2CCCCC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL596055 c5ar1_human Human Yes 4.8 IC50 = 14600 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
443 5 0 3 4.8 Cc1ccc(S(=O)(=O)N(C)c2ccc(Br)cc2C(=O)c2ccccc2)cc1
CHEMBL41547 c5ar1_human Human Yes 7.8 IC50 = 15 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL514872 c5ar1_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
513 6 0 6 5.5 COC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3646922 c5ar1_human Human No 7.8 IC50 = 15 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
494 5 1 5 5.7 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CC(N(C)C)C3)c2C1
CHEMBL41547 c5ar1_human Human Yes 7.8 IC50 = 15.9 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL259971 c5ar1_human Human No 5.8 IC50 = 1500 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
464 6 0 3 7.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1c(C)ccc2ccccc12
CHEMBL516444 c5ar1_human Human No 5.8 IC50 = 1500 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
434 6 1 3 7.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(Cl)ccc1C
CHEMBL421108 c5ar1_human Human No 5.8 IC50 = 1500 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
520 8 4 4 3.1 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(C=Cc4ccccc43)CC2)C1=O
CHEMBL69696 c5ar1_human Human No 5.8 IC50 = 1500 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
536 8 4 5 2.7 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(CC2)CC(=O)c2ccccc23)C1=O
CHEMBL1169838 c5ar1_human Human No 5.8 IC50 = 1584.9 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL3646916 c5ar1_human Human No 7.8 IC50 = 16 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 5 1 5 6.8 CO[C@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@H]1C
CHEMBL3646980 c5ar1_human Human No 7.8 IC50 = 16 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
550 5 1 6 5.8 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(C4COC4)[C@H](C)C3)c2C1
CHEMBL3647024 c5ar1_human Human No 7.8 IC50 = 16 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
545 5 1 8 4.6 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3CC[C@@H](N(C)C)C3)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL3646910 c5ar1_human Human No 6.8 IC50 = 160 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
442 3 0 5 5.2 Cc1ccccc1N1CCc2nc(-c3c(C)cccc3C)nc(N3CCOC(C)(C)C3)c2C1
CHEMBL408391 c5ar1_human Human No 4.8 IC50 = 16000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3646923 c5ar1_human Human No 6.8 IC50 = 163 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
529 4 1 5 6.7 CO[C@@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(Cl)ccc2C)CC3)CC1(C)C
CHEMBL3646937 c5ar1_human Human No 6.8 IC50 = 164 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
534 5 1 5 7.5 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C4CC4)cnc4[nH]ccc34)nc(N3CCCC(C)(C)C3)c2C1
CHEMBL3646930 c5ar1_human Human No 7.8 IC50 = 17 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
538 4 0 5 6.9 CO[C@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(F)(F)F)ccc2C)CC3)CC1(C)C
CHEMBL259563 c5ar1_human Human No 6.8 IC50 = 170 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
450 6 0 3 7.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cccc2ccccc12
CHEMBL260188 c5ar1_human Human No 6.8 IC50 = 170 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
466 6 0 4 7.4 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3c(C)cc(OC)cc3C)cc(OC)c21
CHEMBL259642 c5ar1_human Human No 5.8 IC50 = 1700 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
450 6 0 3 7.9 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3ccccc3C(C)C)cc(OC)c21
CHEMBL409128 c5ar1_human Human No 5.8 IC50 = 1700 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
460 5 0 3 7.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2c(Cl)cccc2C1
CHEMBL1169838 c5ar1_human Human No 5.8 IC50 = 1700 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL604583 c5ar1_human Human No 5.8 IC50 = 1700 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
371 5 0 4 4.1 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)c2ccsc2)cc1
CHEMBL58841 c5ar1_human Human No 4.8 IC50 = 17000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL514872 c5ar1_human Human No 6.8 IC50 = 172 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
513 6 0 6 5.5 COC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL485769 c5ar1_human Human No 6.8 IC50 = 175 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
397 5 0 2 6.6 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)C1CCCCC1
CHEMBL486748 c5ar1_human Human No 6.8 IC50 = 175 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
443 7 0 4 4.9 COCc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL405647 c5ar1_human Human No 7.8 IC50 = 18 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL412031 c5ar1_human Human No 7.8 IC50 = 18 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(C)=O)CCCNC1=O
CHEMBL486953 c5ar1_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
427 6 0 3 5.3 CCc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL3647002 c5ar1_human Human No 7.8 IC50 = 18 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
548 4 1 5 6.1 CC(=O)N1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC12CC2
CHEMBL261278 c5ar1_human Human No 6.8 IC50 = 180 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
480 7 0 4 7.6 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cccc2cc(OC)ccc12
CHEMBL3646988 c5ar1_human Human No 6.8 IC50 = 180 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
384 4 0 2 6.4 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CCN(c1ccc(C)cc1C)C2
CHEMBL118072 c5ar1_human Human No 5.8 IC50 = 1800 nM Bind
50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL259984 c5ar1_human Human No 5.8 IC50 = 1800 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
468 7 0 5 6.8 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3c(OC)cccc3OC)cc(OC)c21
CHEMBL214024 c5ar1_human Human No 7.7 IC50 = 19 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CC#N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3646911 c5ar1_human Human No 7.7 IC50 = 19 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 4 2 5 6.5 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCC(O)C(C)(C)C3)c2C1
CHEMBL513412 c5ar1_human Human No 7.7 IC50 = 20.0 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
470 9 2 6 3.6 COc1ccc(N(C(=O)c2occc2C)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL260176 c5ar1_human Human No 6.7 IC50 = 190 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
480 8 1 4 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CCO)c1cccc2ccccc12
CHEMBL373600 c5ar1_human Human No 6.7 IC50 = 190 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(N)=O
CHEMBL257175 c5ar1_human Human No 5.7 IC50 = 1900 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
440 6 1 3 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@@H]1CCCc2ccccc21
CHEMBL3350744 c5ar1_human Human No 5.7 IC50 = 1949.8 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3647000 c5ar1_human Human No 6.7 IC50 = 197 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
457 7 0 4 6.4 COCCN(C)c1cc(-c2c(C)cccc2C)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL3646998 c5ar1_human Human No 6.7 IC50 = 198 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
362 4 0 6 3.3 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CCN(c1nnnn1C)C2
CHEMBL469728 c5ar1_human Human No 6.7 IC50 = 199.5 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
490 9 2 6 4.0 COc1ccc(N(C(=O)c2occc2Cl)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL1170026 c5ar1_human Human No 5.7 IC50 = 1995.3 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL3350739 c5ar1_human Human No 5.7 IC50 = 1995.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL1628668 c5ar1_human Human Yes 8.7 IC50 = 2 nM Funct
Antagonist activity at C5aR1 in human neutrophils assessed as inhibition of 0.1 nM recombinant human C5a-induced intracellular calcium releaseAntagonist activity at C5aR1 in human neutrophils assessed as inhibition of 0.1 nM recombinant human C5a-induced intracellular calcium release
456 7 0 3 6.5 COc1ccc2c(c1)C(CCC2)C(=O)N(c1ccc(cc1)C(C)C)Cc1ccc(cc1)N(C)C
CHEMBL3646913 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
537 5 1 5 7.2 CO[C@@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646932 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
512 5 0 5 7.0 CO[C@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646936 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
552 5 1 6 6.9 CO[C@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646940 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
526 5 0 6 5.9 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C4(C)COC4)ccc2C)CC3)[C@H](C)C1
CHEMBL3646942 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
486 5 0 6 5.6 COc1ccc(C)c(N2CCc3nc(-c4c(C)cccc4C)nc(N4CC[C@@H](OC)C[C@H]4C)c3C2)c1
CHEMBL3646958 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
578 5 1 6 7.0 CO[C@@H]1CCN(c2nc(-c3c(C(F)(F)F)cnc4[nH]ccc34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646962 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
528 5 1 8 5.1 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)nn2C)CC3)[C@H](C)C1
CHEMBL3646979 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
572 5 1 6 5.4 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(S(C)(=O)=O)[C@H](C)C3)c2C1
CHEMBL3646984 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
572 5 1 6 7.2 CO[C@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(Cl)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3647003 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
562 5 1 8 5.7 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C(C)C)nn2C)CC3)[C@H](C)C1
CHEMBL3647004 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
574 5 1 8 5.7 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL3647011 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
556 5 1 8 5.1 CO[C@@H]1C[C@@H]2CC[C@H](C1)N2c1nc(-c2c(C)ccc3[nH]nc(C)c23)nc2c1CN(c1c(F)c(C3CC3)nn1C)CC2
CHEMBL3647013 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
572 6 1 8 5.6 CCO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(F)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL3647019 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 5 1 6 5.8 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CC[C@@H](N(C)C)C3)c2C1
CHEMBL3647022 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
510 4 1 6 5.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CCOC[C@H]3C)c2C1
CHEMBL3647023 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
532 6 1 8 4.7 CCOC1CN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)C1
CHEMBL3647033 c5ar1_human Human No 8.7 IC50 = 2 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
572 6 1 8 5.7 CCn1nc(C2CC2)c(F)c1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CC[C@@H](OC)C(C)(C)C3)c2C1
CHEMBL41547 c5ar1_human Human Yes 7.7 IC50 = 20 nM Funct
Antagonist activity at C5aR1 in HMDMAntagonist activity at C5aR1 in HMDM
None None None None
CHEMBL3646976 c5ar1_human Human No 7.7 IC50 = 20 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
564 4 1 6 5.1 CC(=O)N1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C4(C)COC4)ccc2C)CC3)[C@H](C)C1
CHEMBL3646996 c5ar1_human Human No 7.7 IC50 = 20 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
426 4 1 5 5.2 Cc1cc(-c2c(C(C)C)ccc3[nH]ncc23)nc2c1CN(c1cc(C3CC3)nn1C)CC2
CHEMBL3647032 c5ar1_human Human No 7.7 IC50 = 20 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
545 6 1 8 4.7 CCn1nc(C2CC2)c(Cl)c1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CC(N(C)C)C3)c2C1
CHEMBL595990 c5ar1_human Human Yes 6.7 IC50 = 200 nM Funct
Antagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
444 6 0 4 4.0 Cc1ccc(S(=O)(=O)N(C)c2ccccc2N(C)S(=O)(=O)c2ccc(C)cc2)cc1
CHEMBL468625 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
540 9 0 5 5.4 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)[C@H](CCN1CCOCC1)Cc1ccc(Cl)cc1
CHEMBL595990 c5ar1_human Human Yes 6.7 IC50 = 200 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
444 6 0 4 4.0 Cc1ccc(S(=O)(=O)N(C)c2ccccc2N(C)S(=O)(=O)c2ccc(C)cc2)cc1
CHEMBL485766 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
413 5 1 3 5.5 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@@H](O)CC1
CHEMBL487141 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
453 5 0 3 6.7 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@@]2(CCCO2)CC1
CHEMBL519730 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
538 8 0 3 7.2 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)C1CCN(CCc2ccc(F)cc2F)CC1
CHEMBL3350745 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
2310 78 32 30 -4.5 CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)C(C)C
CHEMBL1790511 c5ar1_human Human No 6.7 IC50 = 200 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
482 8 3 4 1.9 CC[C@@H](C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL410032 c5ar1_human Human No 5.7 IC50 = 2000 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
468 6 0 2 8.6 CCc1cccc(CC)c1-c1cc(Cl)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL366875 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
331 5 2 2 4.3 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(-c2ccccc2)c1
CHEMBL1170026 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL3350739 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3350744 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL66454 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
482 8 3 4 1.9 CC(C)C[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL307789 c5ar1_human Human No 5.7 IC50 = 2000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
566 8 4 4 3.4 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccc3ccccc3c2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL3646992 c5ar1_human Human No 7.7 IC50 = 21 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
410 3 1 3 6.2 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]nc(C)c34)cc(C)c2C1
CHEMBL468430 c5ar1_human Human No 7.7 IC50 = 22 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
506 7 0 4 5.8 CN(C)CC(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL425469 c5ar1_human Human No 7.7 IC50 = 22 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL481864 c5ar1_human Human No 7.7 IC50 = 22 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
484 7 2 4 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(C(F)(F)F)ccc1CO
CHEMBL3646995 c5ar1_human Human No 7.7 IC50 = 22 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
412 5 0 2 7.2 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CCN(c1cc(C(C)C)ccc1C)C2
CHEMBL259021 c5ar1_human Human No 6.7 IC50 = 220 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
468 7 0 3 7.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2c1CCCC2
CHEMBL302063 c5ar1_human Human No 6.7 IC50 = 220 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
525 9 3 5 2.3 Cc1cccc(C)c1N1CCN(C(=O)[C@@H](CC2CCCCC2)N2C(=O)N[C@H](CCCN=C(N)N)C2=O)CC1
CHEMBL3646939 c5ar1_human Human No 7.6 IC50 = 23 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
498 5 0 5 6.8 CO[C@@H]1CCN(c2nc(-c3cc(C)ccc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3646975 c5ar1_human Human No 7.6 IC50 = 23 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
551 4 0 5 6.2 CC(=O)N1CCN(c2nc(-c3ccccc3C(F)(F)F)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL3647015 c5ar1_human Human No 7.6 IC50 = 23 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
491 6 1 5 6.3 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(OCC(F)F)c2C1
CHEMBL69856 c5ar1_human Human No 6.6 IC50 = 230 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
534 8 4 4 2.4 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccc(F)cc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL431584 c5ar1_human Human No 5.6 IC50 = 2300 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
592 9 4 4 4.0 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL267491 c5ar1_human Human No 4.6 IC50 = 23000 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](C)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL479943 c5ar1_human Human No 5.6 IC50 = 2400 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
431 8 1 4 5.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Oc1ccccc1CCO
CHEMBL480346 c5ar1_human Human No 5.6 IC50 = 2400 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
430 7 1 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccc(OC)cc1C
CHEMBL467571 c5ar1_human Human No 7.6 IC50 = 25 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
484 8 0 4 5.2 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)C(Cc1ccc(Cl)cc1)CN(C)C
CHEMBL374575 c5ar1_human Human No 7.6 IC50 = 25 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(C)=O)CCCNC1=O
CHEMBL405646 c5ar1_human Human No 7.6 IC50 = 25 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@H](C)NC1=O
CHEMBL3647034 c5ar1_human Human No 7.6 IC50 = 25 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
398 3 1 4 5.1 COc1ccc(C)c(N2CCc3nc(-c4c(C)ccc5[nH]ncc45)cc(C)c3C2)c1
CHEMBL68555 c5ar1_human Human No 7.6 IC50 = 25 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
522 8 4 4 3.0 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL471412 c5ar1_human Human No 7.6 IC50 = 25.1 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
476 8 1 4 5.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL479392 c5ar1_human Human No 5.6 IC50 = 2500 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
476 7 1 3 8.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(-c2ccccc2)ccc1C
CHEMBL441305 c5ar1_human Human No 4.6 IC50 = 25000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
339 6 2 3 3.9 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(OC2CCCC2)c1
CHEMBL472455 c5ar1_human Human Yes 6.6 IC50 = 251.2 nM Funct
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay in presence of [35S]GTPgammaSDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay in presence of [35S]GTPgammaS
466 8 1 5 4.9 COc1ccc(N(C(=O)c2ccco2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL375443 c5ar1_human Human No 7.6 IC50 = 26 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL479773 c5ar1_human Human No 7.6 IC50 = 26 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
450 7 2 4 6.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(Cl)ccc1CO
CHEMBL479554 c5ar1_human Human No 5.6 IC50 = 2600 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
460 8 0 5 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cc(OC)ccc1OC
CHEMBL520426 c5ar1_human Human No 5.6 IC50 = 2600 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
448 6 0 3 7.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cc(Cl)ccc1C
CHEMBL3350742 c5ar1_human Human No 5.6 IC50 = 2600 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3350742 c5ar1_human Human No 5.6 IC50 = 2630.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL513344 c5ar1_human Human No 7.6 IC50 = 27 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
499 7 0 5 5.9 COCC(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL259769 c5ar1_human Human No 7.6 IC50 = 27 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
464 7 0 3 7.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL262177 c5ar1_human Human No 7.6 IC50 = 27 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(C)C)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL467571 c5ar1_human Human No 7.6 IC50 = 27 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
484 8 0 4 5.2 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)C(Cc1ccc(Cl)cc1)CN(C)C
CHEMBL3647034 c5ar1_human Human No 7.6 IC50 = 27 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
398 3 1 4 5.1 COc1ccc(C)c(N2CCc3nc(-c4c(C)ccc5[nH]ncc45)cc(C)c3C2)c1
CHEMBL259713 c5ar1_human Human No 6.6 IC50 = 270 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
540 9 0 3 9.5 CCc1cccc(CC)c1-c1cc(OCc2ccccc2)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL262330 c5ar1_human Human No 6.6 IC50 = 270 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
494 5 0 3 7.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2cccc(C(F)(F)F)c2C1
CHEMBL115478 c5ar1_human Human No 6.6 IC50 = 280 nM Bind
50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL41547 c5ar1_human Human Yes 7.5 IC50 = 29 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None None
CHEMBL3646927 c5ar1_human Human No 7.5 IC50 = 29 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
535 5 1 5 6.9 CO[C@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C4CC4)ccc2C)CC3)CC1(C)C
CHEMBL480156 c5ar1_human Human No 6.5 IC50 = 290 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
468 6 1 3 7.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(C(F)(F)F)ccc1C
CHEMBL470384 c5ar1_human Human No 6.5 IC50 = 290 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
445 6 0 6 4.6 COC(=O)C(CC(C)C)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL1170027 c5ar1_human Human No 4.5 IC50 = 29000 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL410692 c5ar1_human Human No 5.5 IC50 = 2951.2 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]1Cc1ccccc1
CHEMBL1628668 c5ar1_human Human Yes 8.5 IC50 = 3 nM Funct
Antagonist activity at C5aR1 in HMDM assessed as inhibition of 1 nM recombinant human C5a-induced intracellular calcium release preincubated for 1 hr followed by human C5a-induction and measured after 60 hrs by FLIPR assayAntagonist activity at C5aR1 in HMDM assessed as inhibition of 1 nM recombinant human C5a-induced intracellular calcium release preincubated for 1 hr followed by human C5a-induction and measured after 60 hrs by FLIPR assay
456 7 0 3 6.5 COc1ccc2c(c1)C(CCC2)C(=O)N(c1ccc(cc1)C(C)C)Cc1ccc(cc1)N(C)C
CHEMBL465377 c5ar1_human Human No 8.5 IC50 = 3 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
521 7 0 5 5.8 CCOC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3646977 c5ar1_human Human No 8.5 IC50 = 3 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
540 6 1 6 5.1 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)cccc3C)nc(N3C[C@H](C)N(CC(N)=O)C[C@H]3C)c2C1
CHEMBL3646994 c5ar1_human Human No 8.5 IC50 = 3 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
438 4 1 3 7.1 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C(C)C)ccc4[nH]ncc34)cc(C)c2C1
CHEMBL3647008 c5ar1_human Human No 8.5 IC50 = 3 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
574 5 1 8 5.7 CO[C@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL41547 c5ar1_human Human Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at C5aR1 in human PMNAntagonist activity at C5aR1 in human PMN
None None None None
CHEMBL480723 c5ar1_human Human No 7.5 IC50 = 30 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
430 8 2 4 5.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1CCO
CHEMBL3646906 c5ar1_human Human No 7.5 IC50 = 30 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
497 7 3 5 6.4 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N[C@@H](CO)C(C)C)c2C1
CHEMBL3646946 c5ar1_human Human No 7.5 IC50 = 30 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
499 5 0 6 6.2 CO[C@@H]1CCN(c2nc(-c3c(C)ccnc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)[C@H](C)C1
CHEMBL308932 c5ar1_human Human No 7.5 IC50 = 30 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
496 9 4 4 2.9 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC(c3ccccc3)CC2)C1=O
CHEMBL41547 c5ar1_human Human Yes 6.5 IC50 = 300 nM Funct
Antagonist activity against the C5a receptorAntagonist activity against the C5a receptor
None None None None
CHEMBL604277 c5ar1_human Human Yes 6.5 IC50 = 300 nM Funct
Antagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
496 10 0 4 5.1 C=CCN(c1ccccc1N(CC=C)S(=O)(=O)c1ccc(C)cc1)S(=O)(=O)c1ccc(C)cc1
CHEMBL374494 c5ar1_human Human No 6.5 IC50 = 300 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CCCCCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(C)=O)CCCNC1=O
CHEMBL604277 c5ar1_human Human Yes 6.5 IC50 = 300 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
496 10 0 4 5.1 C=CCN(c1ccccc1N(CC=C)S(=O)(=O)c1ccc(C)cc1)S(=O)(=O)c1ccc(C)cc1
CHEMBL513055 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
455 5 0 4 5.9 O=C(c1csc2ccccc12)N(CCc1ccccc1Cl)C1CCC2(CC1)OCCO2
CHEMBL291795 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCNC1=O
CHEMBL293241 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCCNC1=O
CHEMBL59355 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL431761 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
525 9 3 5 2.3 Cc1ccc(N2CCN(C(=O)[C@@H](CC3CCCCC3)N3C(=O)N[C@H](CCCN=C(N)N)C3=O)CC2)c(C)c1
CHEMBL68555 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
522 8 4 4 3.0 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL421108 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
520 8 4 4 3.1 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(C=Cc4ccccc43)CC2)C1=O
CHEMBL432533 c5ar1_human Human No 6.5 IC50 = 300 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
536 9 4 4 3.4 N=C(N)NCCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL173206 c5ar1_human Human No 5.5 IC50 = 3000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
337 5 2 2 4.7 C/N=C(/N)Nc1ccc(OCC2CCCCC2)c(-c2ccccc2)c1
CHEMBL3350740 c5ar1_human Human No 5.5 IC50 = 3000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL410692 c5ar1_human Human No 5.5 IC50 = 3000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]1Cc1ccccc1
CHEMBL307127 c5ar1_human Human No 5.5 IC50 = 3000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
468 8 3 4 1.6 CCC[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL68811 c5ar1_human Human No 5.5 IC50 = 3000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
530 9 4 4 2.7 N=C(N)NCCC[C@H]1NC(=O)N(C(CCc2ccccc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL172788 c5ar1_human Human No 4.5 IC50 = 30000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
327 8 3 3 4.0 CCCCOc1ccc(NC(=N)NC)cc1OCc1ccccc1
CHEMBL174463 c5ar1_human Human Yes 4.5 IC50 = 30000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
361 7 2 3 4.2 C/N=C(\N)Nc1ccc(OCc2ccccc2)c(OCc2ccccc2)c1
CHEMBL3350740 c5ar1_human Human No 5.5 IC50 = 3020.0 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3646947 c5ar1_human Human No 6.5 IC50 = 308 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
538 5 0 6 6.1 CO[C@@H]1C[C@@H]2CC[C@H](C1)N2c1nc(-c2c(C)cccc2C)nc2c1CN(c1cc(C3(C)COC3)ccc1C)CC2
CHEMBL435580 c5ar1_human Human No 5.5 IC50 = 3090.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCNC1=O
CHEMBL41547 c5ar1_human Human Yes 7.5 IC50 = 31 nM Funct
Antagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase releaseAntagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase release
None None None None
CHEMBL376905 c5ar1_human Human No 7.5 IC50 = 31 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL463115 c5ar1_human Human No 7.5 IC50 = 31 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
553 6 1 3 7.2 O=C(Nc1ccc(F)cc1F)N1CCC(N(CCc2ccc(Cl)cc2)C(=O)c2csc3ccccc23)CC1
CHEMBL3639458 c5ar1_human Human No 7.5 IC50 = 31 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
509 5 0 6 6.2 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C#N)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@H]1C
CHEMBL3646914 c5ar1_human Human No 7.5 IC50 = 31 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
509 4 2 5 6.1 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CC[C@H](O)[C@H](C)C3)c2C1
CHEMBL3646967 c5ar1_human Human No 7.5 IC50 = 31 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
526 6 1 6 4.8 Cc1ccc(C)c(-c2nc3c(c(N4CCN(CC(N)=O)C[C@H]4C)n2)CN(c2cc(C(C)C)ccc2C)CC3)c1
CHEMBL3647016 c5ar1_human Human No 7.5 IC50 = 31 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
484 7 2 6 5.2 CNCCOc1nc(-c2c(C)ccc3[nH]nc(C)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL471412 c5ar1_human Human No 7.5 IC50 = 31.6 nM Funct
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay in presence of [35S]GTPgammaSDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay in presence of [35S]GTPgammaS
476 8 1 4 5.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL604583 c5ar1_rat Rat No 5.5 IC50 = 3100 nM Funct
Antagonist activity at C5a receptor in rat RAW264.7 cells assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at C5a receptor in rat RAW264.7 cells assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
371 5 0 4 4.1 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)c2ccsc2)cc1
CHEMBL435580 c5ar1_human Human No 5.5 IC50 = 3100 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCNC1=O
CHEMBL513370 c5ar1_human Human No 6.5 IC50 = 316.2 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
490 9 2 6 4.0 COc1ccc(N(C(=O)c2ccoc2Cl)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL512543 c5ar1_human Human No 5.5 IC50 = 3162.3 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
513 11 2 7 3.4 COc1ccc(N(C(=O)c2occc2CN(C)C)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL472455 c5ar1_human Human Yes 5.5 IC50 = 3162.3 nM Bind
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assayDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay
466 8 1 5 4.9 COc1ccc(N(C(=O)c2ccco2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL1170027 c5ar1_human Human No 4.5 IC50 = 31622.8 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL465377 c5ar1_human Human No 7.5 IC50 = 32 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
521 7 0 5 5.8 CCOC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3647017 c5ar1_human Human No 7.5 IC50 = 32 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
540 7 1 7 5.3 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(OCCN3CCOCC3)c2C1
CHEMBL334290 c5ar1_human Human No 5.5 IC50 = 3200 nM Bind
50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL480318 c5ar1_human Human No 5.5 IC50 = 3200 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
416 5 0 4 6.2 COc1ccc(C)c(N(C)C2CCCc3nc(-c4c(C)cccc4C)cc(OC)c32)c1
CHEMBL291589 c5ar1_human Human No 5.5 IC50 = 3200 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCCNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL291589 c5ar1_human Human No 5.5 IC50 = 3235.9 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCCNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL459090 c5ar1_human Human No 6.5 IC50 = 325 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
424 2 0 5 6.4 Clc1cccc2nc(-c3csc4ccccc34)n(C3CCC4(CC3)OCCO4)c12
CHEMBL519401 c5ar1_human Human No 6.5 IC50 = 330 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
552 7 0 3 6.8 O=C(Cc1ccc(F)cc1F)N1CCC(N(CCc2ccc(Cl)cc2)C(=O)c2csc3ccccc23)CC1
CHEMBL3646903 c5ar1_human Human No 6.5 IC50 = 338 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
460 4 1 7 4.1 Cc1cccc(C)c1-c1nc2c(c(N3CCCC(O)C3)n1)CN(c1cc(C(C)C)nn1C)CC2
CHEMBL479558 c5ar1_human Human No 6.5 IC50 = 340 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
431 7 0 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Oc1cc(OC)ccc1C
CHEMBL69192 c5ar1_human Human No 5.5 IC50 = 3400 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
500 9 3 5 1.6 CSCC[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL471210 c5ar1_human Human No 7.5 IC50 = 35 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
469 5 0 4 6.5 CC(CN(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2)c1ccc(Cl)cc1
CHEMBL408460 c5ar1_human Human No 6.5 IC50 = 350 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
422 5 0 3 7.1 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3ccccc3C)cc(OC)c21
CHEMBL456250 c5ar1_human Human No 6.5 IC50 = 350 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
471 7 1 4 4.7 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)C(Cc1ccc(Cl)cc1)C(=O)O
CHEMBL486971 c5ar1_human Human No 6.5 IC50 = 350 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
411 5 0 3 5.8 O=C1CCC(N(CCc2ccc(Cl)cc2)C(=O)c2csc3ccccc23)CC1
CHEMBL420736 c5ar1_human Human No 6.5 IC50 = 350 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
511 9 3 5 2.0 Cc1ccccc1N1CCN(C(=O)[C@@H](CC2CCCCC2)N2C(=O)N[C@H](CCCN=C(N)N)C2=O)CC1
CHEMBL479557 c5ar1_human Human No 5.5 IC50 = 3500 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
417 7 2 5 5.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cnccc1CO
CHEMBL3350737 c5ar1_human Human No 5.5 IC50 = 3548.1 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL415150 c5ar1_human Human No 6.4 IC50 = 360 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3350737 c5ar1_human Human No 5.4 IC50 = 3600 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL258797 c5ar1_human Human No 7.4 IC50 = 37 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
518 8 0 3 9.3 CCc1cccc(CC)c1-c1cc(OC2CCCC2)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL3646990 c5ar1_human Human No 7.4 IC50 = 37 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
400 3 1 5 4.6 CCn1nc(C)c(N2CCc3nc(-c4c(C)ccc5[nH]ncc45)cc(C)c3C2)c1C
CHEMBL519705 c5ar1_human Human No 6.4 IC50 = 370 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
405 6 0 2 6.4 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)Cc1ccccc1
CHEMBL374717 c5ar1_human Human No 7.4 IC50 = 38 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](C2CCCCC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3639459 c5ar1_human Human No 7.4 IC50 = 38 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
381 2 1 2 6.0 Cc1cc(-c2cccc3[nH]cc(C)c23)nc2c1CN(c1c(C)cccc1C)CC2
CHEMBL518297 c5ar1_human Human No 6.4 IC50 = 380 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
450 7 1 4 7.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(OC)ccc1Cl
CHEMBL433838 c5ar1_human Human No 5.4 IC50 = 3800 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCNC1=O
CHEMBL433838 c5ar1_human Human No 5.4 IC50 = 3801.9 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCNC1=O
CHEMBL603858 c5ar1_human Human Yes 4.4 IC50 = 38300 nM Funct
Antagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
406 4 0 3 4.0 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)N2CCc3ccccc32)cc1
CHEMBL2371928 c5ar1_human Human No 7.4 IC50 = 39 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL3646920 c5ar1_human Human No 7.4 IC50 = 39 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
495 5 2 5 5.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCC[C@@H]3CO)c2C1
CHEMBL472268 c5ar1_human Human No 7.4 IC50 = 39.8 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
470 9 2 6 3.6 COc1ccc(N(C(=O)c2ccoc2C)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL471412 c5ar1_human Human No 7.4 IC50 = 39.8 nM Bind
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by whole cell binding assayDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by whole cell binding assay
476 8 1 4 5.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL511613 c5ar1_human Human No 6.4 IC50 = 395 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
407 4 0 4 5.2 O=C(c1csc2ccccc12)N(Cc1ccccc1)C1CCC2(CC1)OCCO2
CHEMBL3646904 c5ar1_human Human Yes 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
289 3 0 4 2.7 COc1nc(Cl)nc2c1CN(Cc1ccccc1)CC2
CHEMBL3646924 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
550 5 1 6 6.8 CO[C@@H]1C[C@@H]2CC[C@H](C1)N2c1nc(-c2c(C)ccc3[nH]nc(C)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL3646931 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
594 6 1 7 6.6 CO[C@H]1CCN(c2nc(-c3c(C(C)C)ccc4[nH]ncc34)nc3c2CN(c2cc(C4(C)COC4)ccc2C)CC3)CC1(C)C
CHEMBL3646933 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
554 6 1 7 6.3 COc1ccc(C)c(N2CCc3nc(-c4c(C(C)C)ccc5[nH]ncc45)nc(N4CC[C@H](OC)C(C)(C)C4)c3C2)c1
CHEMBL3646935 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
518 5 0 5 7.0 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3Cl)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@H]1C
CHEMBL3646948 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
538 4 0 5 6.9 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(F)(F)F)ccc2C)CC3)CC1(C)C
CHEMBL3646950 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
555 5 1 5 7.3 CO[C@H]1CCN(c2nc(-c3ccc(F)c4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646978 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
565 6 2 6 5.3 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3C[C@H](C)N(CC(N)=O)C[C@H]3C)c2C1
CHEMBL3647004 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
574 5 1 8 5.7 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL3647005 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
588 6 1 8 6.1 CCO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)CC1(C)C
CHEMBL3647020 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
553 6 1 7 5.4 COC1CN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@@H]1N(C)C
CHEMBL3647025 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
518 4 2 8 4.0 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3C[C@@H](O)[C@@H]3C)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL3647026 c5ar1_human Human No 8.4 IC50 = 4 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
532 5 1 8 4.7 CO[C@@H]1CN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)[C@H]1C
CHEMBL513964 c5ar1_human Human No 7.4 IC50 = 40 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
509 7 0 6 5.7 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)C(Cc1ccc(Cl)cc1)c1noc(C)n1
CHEMBL3646959 c5ar1_human Human No 7.4 IC50 = 40 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
488 5 0 7 5.2 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(C)C)nn2C)CC3)[C@H](C)C1
CHEMBL302063 c5ar1_human Human No 7.4 IC50 = 40 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
525 9 3 5 2.3 Cc1cccc(C)c1N1CCN(C(=O)[C@@H](CC2CCCCC2)N2C(=O)N[C@H](CCCN=C(N)N)C2=O)CC1
CHEMBL420736 c5ar1_human Human No 7.4 IC50 = 40 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
511 9 3 5 2.0 Cc1ccccc1N1CCN(C(=O)[C@@H](CC2CCCCC2)N2C(=O)N[C@H](CCCN=C(N)N)C2=O)CC1
CHEMBL604583 c5ar1_human Human No 6.4 IC50 = 400 nM Funct
Antagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
371 5 0 4 4.1 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)c2ccsc2)cc1
CHEMBL513247 c5ar1_human Human No 6.4 IC50 = 400 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
450 5 0 4 5.3 O=C(c1cncc2ccccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL308932 c5ar1_human Human No 6.4 IC50 = 400 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
496 9 4 4 2.9 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC(c3ccccc3)CC2)C1=O
CHEMBL170859 c5ar1_human Human No 5.4 IC50 = 4000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
347 6 2 3 4.4 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(Oc2ccccc2)c1
CHEMBL171630 c5ar1_human Human No 5.4 IC50 = 4000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
403 10 2 3 5.0 C/N=C(/N)Nc1ccc(OCCCCc2ccccc2)c(OCc2ccccc2)c1
CHEMBL303940 c5ar1_human Human No 5.4 IC50 = 4000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
532 8 5 5 2.0 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccc(O)cc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL306210 c5ar1_human Human No 5.4 IC50 = 4000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
494 8 2 4 3.9 NCCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL70043 c5ar1_human Human No 5.4 IC50 = 4000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
516 8 4 4 2.3 N=C(N)NCCC[C@@H]1NC(=O)N([C@H](Cc2ccccc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL2371928 c5ar1_human Human No 7.4 IC50 = 41 nM Funct
Antagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase releaseAntagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase release
None None None CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL480783 c5ar1_human Human No 6.4 IC50 = 410 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
430 7 2 4 6.1 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1C(=O)O
CHEMBL408492 c5ar1_human Human No 4.4 IC50 = 41000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CNC1=O
CHEMBL3646921 c5ar1_human Human No 6.4 IC50 = 415 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
493 4 1 5 5.8 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CC4(COC4)C3)c2C1
CHEMBL3646997 c5ar1_human Human No 7.4 IC50 = 42 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
460 4 1 5 5.9 Cc1cc(-c2c(C(C)C)ccc3[nH]ncc23)nc2c1CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL472136 c5ar1_human Human No 6.4 IC50 = 420 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
446 8 1 5 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(OC)ccc1OC
CHEMBL517683 c5ar1_human Human No 6.4 IC50 = 430 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
414 6 1 3 7.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(C)ccc1C
CHEMBL58617 c5ar1_human Human No 4.4 IC50 = 43000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O
CHEMBL469528 c5ar1_human Human No 6.4 IC50 = 435 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
471 6 0 5 5.8 O=C(c1csc2ccccc12)N(CCOc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL603858 c5ar1_human Human Yes 4.4 IC50 = 44500 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
406 4 0 3 4.0 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)N2CCc3ccccc32)cc1
CHEMBL425289 c5ar1_human Human No 7.4 IC50 = 45 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CC2CCCCC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL468429 c5ar1_human Human No 7.4 IC50 = 45 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
497 6 0 5 5.9 CC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL303711 c5ar1_human Human No 6.4 IC50 = 450 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
555 8 5 4 2.8 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL66454 c5ar1_human Human No 6.4 IC50 = 450 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
482 8 3 4 1.9 CC(C)C[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O
CHEMBL425497 c5ar1_human Human No 5.4 IC50 = 4500 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
381 5 2 2 5.4 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(-c2cccc3ccccc23)c1
CHEMBL3350735 c5ar1_human Human No 5.3 IC50 = 4570.9 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3646917 c5ar1_human Human No 7.3 IC50 = 46 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
535 5 1 5 7.1 CO[C@@H]1C[C@@H]2CC[C@H](C1)N2c1nc(-c2cccc3[nH]cc(C)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL260175 c5ar1_human Human No 5.3 IC50 = 4600 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
426 5 0 3 7.0 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3ccccc3F)cc(OC)c21
CHEMBL3350735 c5ar1_human Human No 5.3 IC50 = 4600 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NCCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL374120 c5ar1_human Human No 6.3 IC50 = 463 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CCCC[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(N)=O
CHEMBL3646971 c5ar1_human Human No 6.3 IC50 = 464 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
531 5 2 6 3.8 Cc1c[nH]c2cccc(-c3nc4c(c(N5CCN(CC(N)=O)[C@H](C)C5)n3)CN(c3ccc(F)cc3F)CC4)c12
CHEMBL457790 c5ar1_human Human No 7.3 IC50 = 47 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
436 4 0 5 6.7 c1ccc2c(-c3ncc(CC4CCCCC4)n3C3CCC4(CC3)OCCO4)csc2c1
CHEMBL3646929 c5ar1_human Human No 7.3 IC50 = 47 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
556 5 1 6 6.7 CO[C@H]1CCN(c2nc(-c3c(Cl)cnc4[nH]ccc34)nc3c2CN(c2cc(C4CC4)ccc2C)CC3)CC1(C)C
CHEMBL1170029 c5ar1_human Human No 5.3 IC50 = 4700 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL3350734 c5ar1_human Human No 5.3 IC50 = 4786.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3646901 c5ar1_human Human No 7.3 IC50 = 48 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
472 4 0 6 5.8 Cc1cccc(C)c1-c1nc2c(c(N3CCCC(C)(C)C3)n1)CN(c1cc(C(C)C)nn1C)CC2
CHEMBL3350734 c5ar1_human Human No 5.3 IC50 = 4800 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3647035 c5ar1_human Human No 7.3 IC50 = 49 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
410 3 1 3 6.2 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]ncc34)cc(C)c2C1
CHEMBL219236 c5ar1_human Human No 6.3 IC50 = 490 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL519456 c5ar1_human Human No 5.3 IC50 = 4900 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
411 6 1 4 6.2 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1C#N
CHEMBL471017 c5ar1_human Human No 8.3 IC50 = 5 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
527 7 0 6 5.9 CCOC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL520715 c5ar1_human Human No 8.3 IC50 = 5 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
453 5 0 3 6.7 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@]2(CCCO2)CC1
CHEMBL3646955 c5ar1_human Human No 8.3 IC50 = 5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
524 4 0 5 6.7 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C(F)(F)F)ccc2C)CC3)[C@H](C)C1
CHEMBL3646961 c5ar1_human Human No 8.3 IC50 = 5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
556 6 1 8 5.8 CO[C@H]1CCN(c2nc(-c3c(C(C)C)ccc4[nH]ncc34)nc3c2CN(c2cc(C(C)C)nn2C)CC3)CC1(C)C
CHEMBL3646974 c5ar1_human Human No 8.3 IC50 = 5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
534 4 1 5 5.7 CC(=O)N1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C4CC4)ccc2C)CC3)[C@H](C)C1
CHEMBL3647007 c5ar1_human Human No 8.3 IC50 = 5 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
574 6 1 8 5.9 CCO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C4CC4)nn2C)CC3)[C@H](C)C1
CHEMBL375137 c5ar1_human Human No 7.3 IC50 = 50 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(C)=O)CCCNC1=O
CHEMBL116851 c5ar1_human Human No 6.3 IC50 = 500 nM Bind
50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(N)=O
CHEMBL456053 c5ar1_human Human No 6.3 IC50 = 500 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
464 4 0 5 6.9 Clc1ccc(Cc2cnc(-c3csc4ccccc34)n2C2CCC3(CC2)OCCO3)cc1
CHEMBL468626 c5ar1_human Human No 6.3 IC50 = 500 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
456 7 0 4 4.8 CN(C)Cc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL481357 c5ar1_human Human No 5.3 IC50 = 5000 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
415 7 2 4 5.8 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1CN
CHEMBL303711 c5ar1_human Human No 5.3 IC50 = 5000 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
555 8 5 4 2.8 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL71506 c5ar1_human Human No 5.3 IC50 = 5000 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
604 9 4 4 4.8 N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCC(C3CCCCC3)CC2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL169553 c5ar1_human Human No 4.3 IC50 = 50000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
365 5 2 2 4.9 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(-c2ccc(Cl)cc2)c1
CHEMBL1170025 c5ar1_human Human No 6.3 IC50 = 501.2 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL1170029 c5ar1_human Human No 5.3 IC50 = 5011.9 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
CHEMBL374542 c5ar1_human Human No 7.3 IC50 = 51 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3350741 c5ar1_human Human No 4.3 IC50 = 51000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](CC1c2ccccc2-c2ccccc21)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL479394 c5ar1_human Human No 7.3 IC50 = 53 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
434 7 2 4 6.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccc(F)cc1CO
CHEMBL261277 c5ar1_human Human No 6.3 IC50 = 530 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
480 7 0 4 7.6 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccc(OC)c2ccccc12
CHEMBL409977 c5ar1_human Human No 6.3 IC50 = 535 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL413916 c5ar1_human Human No 7.3 IC50 = 54 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3646909 c5ar1_human Human No 7.3 IC50 = 54 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
372 3 0 4 4.7 Cc1ccccc1N1CCc2nc(-c3c(C)cccc3C)nc(N(C)C)c2C1
CHEMBL173708 c5ar1_human Human No 4.3 IC50 = 54000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
361 6 3 3 4.5 CNC(=N)Nc1ccc(OCc2ccccc2)c(-c2ccc(OC)cc2)c1
CHEMBL3646993 c5ar1_human Human No 6.3 IC50 = 550 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
420 4 0 3 6.7 COc1ccc(Cl)c(-c2cc(C)c3c(n2)CCN(c2cc(C(C)C)ccc2C)C3)c1
CHEMBL257128 c5ar1_human Human No 5.3 IC50 = 5500 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
440 6 1 3 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@H]1CCCc2ccccc21
CHEMBL407285 c5ar1_human Human No 4.3 IC50 = 55000 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](C)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3646941 c5ar1_human Human No 7.3 IC50 = 56 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
513 5 0 6 6.4 CO[C@@H]1CCN(c2nc(-c3c(C)cncc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3647035 c5ar1_human Human No 7.3 IC50 = 56 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
410 3 1 3 6.2 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]ncc34)cc(C)c2C1
CHEMBL3647036 c5ar1_human Human No 7.3 IC50 = 56 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
385 3 1 4 4.9 CCn1cc(N2CCc3nc(-c4cccc5[nH]cc(C)c45)cc(C)c3C2)c(C)n1
CHEMBL480892 c5ar1_human Human No 6.3 IC50 = 560 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
444 7 0 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cc(OC)ccc1C
CHEMBL1170025 c5ar1_human Human No 6.3 IC50 = 560 nM Bind
Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting
None None None None
CHEMBL435921 c5ar1_human Human No 7.2 IC50 = 57 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL435927 c5ar1_human Human No 6.2 IC50 = 570 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCC/N=C(/N)N[N+](=O)[O-])NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3647037 c5ar1_human Human No 7.2 IC50 = 58 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
414 5 0 4 5.7 CCc1cccc(CC)c1-c1cc(C)c2c(n1)CC(C)N(c1cc(C3CC3)nn1C)C2
CHEMBL3350738 c5ar1_human Human No 5.2 IC50 = 5888.4 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte(PMN) C5a anaphylatoxin chemotactic receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte(PMN) C5a anaphylatoxin chemotactic receptor
None None None NC(N)=NCCC[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)O
CHEMBL604277 c5ar1_human Human Yes 7.2 IC50 = 59 nM Funct
Antagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
496 10 0 4 5.1 C=CCN(c1ccccc1N(CC=C)S(=O)(=O)c1ccc(C)cc1)S(=O)(=O)c1ccc(C)cc1
CHEMBL408458 c5ar1_human Human No 5.2 IC50 = 5900 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
458 5 0 3 8.0 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3cccc4ccccc34)cc(OC)c21
CHEMBL3350738 c5ar1_human Human No 5.2 IC50 = 5900 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte(PMN) C5a anaphylatoxin chemotactic receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte(PMN) C5a anaphylatoxin chemotactic receptor
None None None NC(N)=NCCC[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)O
CHEMBL3646954 c5ar1_human Human No 8.2 IC50 = 6 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
578 4 1 6 6.8 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(F)(F)F)ccc2C)CC3)CC1(C)C
CHEMBL3646973 c5ar1_human Human No 8.2 IC50 = 6 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
552 6 2 7 4.3 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)ccc4[nH]ncc34)nc(N3CCN(CC(N)=O)C[C@H]3C)c2C1
CHEMBL3646983 c5ar1_human Human No 8.2 IC50 = 6 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
461 4 1 5 6.0 COc1nc(-c2c(C)ccc3[nH]nc(Cl)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL3647010 c5ar1_human Human No 8.2 IC50 = 6 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
602 4 1 8 5.9 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2c(Cl)c(C(F)(F)F)nn2C)CC3)CC1(C)C
CHEMBL595990 c5ar1_human Human Yes 8.2 IC50 = 6.7 nM Funct
Antagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at C5a receptor in human PMNC assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
444 6 0 4 4.0 Cc1ccc(S(=O)(=O)N(C)c2ccccc2N(C)S(=O)(=O)c2ccc(C)cc2)cc1
CHEMBL437988 c5ar1_human Human No 7.2 IC50 = 60 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(C)C)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL62201 c5ar1_human Human No 7.2 IC50 = 60 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCNC1=O
CHEMBL431761 c5ar1_human Human No 7.2 IC50 = 60 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
525 9 3 5 2.3 Cc1ccc(N2CCN(C(=O)[C@@H](CC3CCCCC3)N3C(=O)N[C@H](CCCN=C(N)N)C3=O)CC2)c(C)c1
CHEMBL604583 c5ar1_human Human No 6.2 IC50 = 600 nM Funct
Antagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assayAntagonist activity at human C5a receptor expressed in CHO cells co-expressed with Galpha16 assessed as inhibition of anaphylatoxin C5a-induced intracellular calcium accumulation after 10 mins by FLIPR assay
371 5 0 4 4.1 Cc1ccc(S(=O)(=O)N(C)c2ccccc2C(=O)c2ccsc2)cc1
CHEMBL355676 c5ar1_human Human No 5.2 IC50 = 6000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
389 9 2 3 4.6 C/N=C(/N)Nc1ccc(OCCCc2ccccc2)c(OCc2ccccc2)c1
CHEMBL260472 c5ar1_human Human No 5.2 IC50 = 6200 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
478 6 0 3 7.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C(C)=O)c1cccc2ccccc12
CHEMBL479543 c5ar1_human Human No 5.2 IC50 = 6200 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
444 7 0 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccc(OC)cc1C
CHEMBL409045 c5ar1_human Human No 7.2 IC50 = 63 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL511782 c5ar1_human Human No 7.2 IC50 = 63.1 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
466 9 2 5 3.7 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC[C@@H](C)O)c2ccccc2F)c(OC)c1
CHEMBL3646966 c5ar1_human Human No 7.2 IC50 = 64 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
568 4 1 8 5.2 CO[C@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(F)(F)F)nn2C)CC3)CC1(C)C
CHEMBL3646925 c5ar1_human Human No 7.2 IC50 = 65 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
550 5 0 5 7.2 CO[C@H]1CCN(c2nc(-c3ccccc3C(F)(F)F)nc3c2CN(c2cc(C4CC4)ccc2C)CC3)CC1(C)C
CHEMBL259643 c5ar1_human Human No 6.2 IC50 = 650 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
436 6 0 3 7.4 CCc1ccccc1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL261276 c5ar1_human Human No 7.2 IC50 = 67 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
478 8 0 3 8.3 CCOc1cc(-c2c(CC)cccc2CC)nc2c1C(N(CC)c1cccc3ccccc13)CCC2
CHEMBL3647027 c5ar1_human Human No 7.2 IC50 = 67 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
531 5 1 8 4.2 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3CC(N(C)C)C3)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL480891 c5ar1_human Human No 6.2 IC50 = 690 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
428 6 0 3 7.0 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cc(C)ccc1C
CHEMBL214456 c5ar1_human Human No 5.2 IC50 = 6900 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL479372 c5ar1_human Human No 8.2 IC50 = 7 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
458 9 2 4 6.7 CCc1cccc(CC)c1-c1cc(OC(C)C)c2c(n1)CCCC2Nc1ccccc1CCO
CHEMBL3646943 c5ar1_human Human No 8.2 IC50 = 7 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
490 4 0 5 6.3 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(Cl)ccc2C)CC3)[C@H](C)C1
CHEMBL3646970 c5ar1_human Human No 8.2 IC50 = 7 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
577 5 2 6 4.8 Cc1ccc(C(F)(F)F)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(CC(N)=O)[C@H](C)C3)c2C1
CHEMBL487167 c5ar1_human Human No 7.2 IC50 = 70 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
413 5 1 3 5.5 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1
CHEMBL117143 c5ar1_human Human No 6.2 IC50 = 700 nM Bind
50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
None None None CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL262181 c5ar1_human Human No 7.2 IC50 = 71 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(C)C)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O
CHEMBL479395 c5ar1_human Human No 7.2 IC50 = 71 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
450 7 2 4 6.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccc(Cl)cc1CO
CHEMBL479540 c5ar1_human Human No 6.1 IC50 = 730 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
414 7 1 3 6.9 CCc1ccccc1NC1CCCc2nc(-c3c(CC)cccc3CC)cc(OC)c21
CHEMBL3646986 c5ar1_human Human No 7.1 IC50 = 74 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
459 8 0 5 6.2 COCCCOc1nc(-c2c(C)cccc2C)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL517693 c5ar1_human Human No 5.1 IC50 = 7400 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
416 7 1 4 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cccc(OC)c1
CHEMBL3646926 c5ar1_human Human No 6.1 IC50 = 746 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
566 5 0 8 5.4 CO[C@H]1CCN(c2nc(-c3cccc4cnn(C)c34)nc3c2CN(c2cc(C4(C)COC4)ccc2C)CC3)CC1(C)C
CHEMBL519540 c5ar1_human Human No 7.1 IC50 = 75 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
455 5 0 4 5.9 O=C(c1csc2ccccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL3646969 c5ar1_human Human No 7.1 IC50 = 75 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
527 5 2 6 3.9 Cc1ccc(F)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(CC(N)=O)[C@H](C)C3)c2C1
CHEMBL171211 c5ar1_human Human No 5.1 IC50 = 7500 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
375 8 2 3 4.2 C/N=C(/N)Nc1ccc(OCCc2ccccc2)c(OCc2ccccc2)c1
CHEMBL374694 c5ar1_human Human No 7.1 IC50 = 76 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
936 11 7 7 4.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL3646981 c5ar1_human Human No 7.1 IC50 = 77 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
469 4 1 6 4.8 COc1nc(-c2c(C)ccc3[nH]nc(C)c23)nc2c1CN(c1cc(C3(C)COC3)ccc1C)CC2
CHEMBL3647041 c5ar1_human Human No 7.1 IC50 = 78 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
409 3 1 2 6.8 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)cc(C)c2C1
CHEMBL3646985 c5ar1_human Human No 7.1 IC50 = 79 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
484 5 0 5 6.1 COC1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN([C@@H](C)c2ccccc2)CC3)CC1(C)C
CHEMBL472455 c5ar1_human Human Yes 7.1 IC50 = 79.4 nM Bind
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by whole cell binding assayDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by whole cell binding assay
466 8 1 5 4.9 COc1ccc(N(C(=O)c2ccco2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL481295 c5ar1_human Human No 6.1 IC50 = 790 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
414 6 0 3 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccccc1C
CHEMBL459092 c5ar1_human Human No 6.1 IC50 = 790 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
458 2 0 5 7.1 Clc1ccc2nc(-c3csc4ccccc34)n(C3CCC4(CC3)OCCO4)c2c1Cl
CHEMBL3646999 c5ar1_human Human No 6.1 IC50 = 790 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
471 7 0 4 6.1 COCCN(C)c1cc(-c2c(C)cccc2C)nc2c1C(=O)N(c1cc(C(C)C)ccc1C)CC2
CHEMBL410927 c5ar1_human Human No 5.1 IC50 = 7900 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
400 6 0 3 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccccc1
CHEMBL410927 c5ar1_human Human No 5.1 IC50 = 7900 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
400 6 0 3 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccccc1
CHEMBL450470 c5ar1_human Human No 6.1 IC50 = 794.3 nM Funct
Antagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilizationAntagonist activity at human recombinant C5a receptor in HEK cells assessed as inhibition of C5a-induced calcium mobilization
414 7 1 4 4.0 COc1ccc(N(C(C)=O)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL471412 c5ar1_human Human No 6.1 IC50 = 794.3 nM Bind
Displacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assayDisplacement of [Alexa647]C5a from human recombinant C5a receptor expressed in HEK cells by membrane binding assay
476 8 1 4 5.3 COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1
CHEMBL3350743 c5ar1_human Human No 6.1 IC50 = 794.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL513964 c5ar1_human Human No 8.1 IC50 = 8 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
509 7 0 6 5.7 CCc1ccccc1C(=O)N(C1CCC2(CC1)OCCO2)C(Cc1ccc(Cl)cc1)c1noc(C)n1
CHEMBL3646960 c5ar1_human Human No 8.1 IC50 = 8 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
486 5 0 7 4.9 CO[C@@H]1CCN(c2nc(-c3c(C)cccc3C)nc3c2CN(c2cc(C4CC4)nn2C)CC3)[C@H](C)C1
CHEMBL3646965 c5ar1_human Human No 8.1 IC50 = 8 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
554 4 1 8 5.0 CO[C@@H]1CCN(c2nc(-c3c(C)ccc4[nH]nc(C)c34)nc3c2CN(c2cc(C(F)(F)F)nn2C)CC3)[C@H](C)C1
CHEMBL3646972 c5ar1_human Human No 8.1 IC50 = 8 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
551 6 2 6 4.9 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3cccc4[nH]cc(C)c34)nc(N3CCN(CC(N)=O)[C@H](C)C3)c2C1
CHEMBL3647029 c5ar1_human Human No 8.1 IC50 = 8 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
544 4 1 8 4.7 Cc1ccc2[nH]nc(C)c2c1-c1nc2c(c(N3CC[C@H]4OC[C@H]4C3)n1)CN(c1c(Cl)c(C3CC3)nn1C)CC2
CHEMBL488388 c5ar1_human Human No 7.1 IC50 = 80 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
449 5 0 3 5.9 O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL368161 c5ar1_human Human No 6.1 IC50 = 800 nM Funct
Compound was evaluated for the antagonistic activity against C5a anaphylatoxin chemotactic receptor in human neutrophil C5a stimulated respiratory burst assayCompound was evaluated for the antagonistic activity against C5a anaphylatoxin chemotactic receptor in human neutrophil C5a stimulated respiratory burst assay
345 6 2 2 4.3 CN=C(Nc1ccc(c(c1)c1ccccc1)OCCc1ccccc1)N
CHEMBL3350743 c5ar1_human Human No 6.1 IC50 = 800 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL71841 c5ar1_human Human No 6.1 IC50 = 800 nM Bind
Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations
516 8 4 4 2.3 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccccc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL174374 c5ar1_human Human No 5.1 IC50 = 8000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
349 5 2 2 4.4 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(-c2cccc(F)c2)c1
CHEMBL353857 c5ar1_human Human No 5.1 IC50 = 8000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
367 7 2 3 4.6 C/N=C(/N)Nc1ccc(OCC2CCCCC2)c(OCc2ccccc2)c1
CHEMBL71841 c5ar1_human Human No 5.1 IC50 = 8000 nM Bind
Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
516 8 4 4 2.3 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccccc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL3647040 c5ar1_human Human No 6.1 IC50 = 802 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
410 3 1 3 6.2 Cc1ccc(C(C)C)cc1N1CCc2nc(-c3c(C)cnc4[nH]ccc34)cc(C)c2C1
CHEMBL257175 c5ar1_human Human No 5.1 IC50 = 8100 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
440 6 1 3 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@@H]1CCCc2ccccc21
CHEMBL435777 c5ar1_human Human No 5.1 IC50 = 8100 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCCNC1=O
CHEMBL435777 c5ar1_human Human No 5.1 IC50 = 8128.3 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None NC(N)=NCC[C@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CCCCNC1=O
CHEMBL408432 c5ar1_human Human No 7.1 IC50 = 82 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
480 7 0 3 8.7 CCc1cccc(CC)c1-c1cc(SC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL257128 c5ar1_human Human No 6.1 IC50 = 820 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
440 6 1 3 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@H]1CCCc2ccccc21
CHEMBL520381 c5ar1_human Human No 6.1 IC50 = 835 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
458 7 0 5 4.9 CC(C)Oc1ncccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2
CHEMBL261594 c5ar1_human Human No 6.1 IC50 = 840 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
484 6 0 5 6.1 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2cccc(C(=O)OC)c2C1
CHEMBL457790 c5ar1_human Human No 6.1 IC50 = 850 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
436 4 0 5 6.7 c1ccc2c(-c3ncc(CC4CCCCC4)n3C3CCC4(CC3)OCCO4)csc2c1
CHEMBL3646991 c5ar1_human Human No 6.1 IC50 = 868 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
398 3 1 5 4.4 Cc1cc(-c2c(C)ccc3[nH]ncc23)nc2c1CN(c1cc(C3CC3)nn1C)CC2
CHEMBL412008 c5ar1_human Human No 5.1 IC50 = 8700 nM Funct
Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase releaseAntagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL595824 c5ar1_human Human Yes 5.1 IC50 = 8700 nM Bind
Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr
399 5 0 3 4.7 Cc1ccc(S(=O)(=O)N(C)c2ccc(Cl)cc2C(=O)c2ccccc2)cc1
CHEMBL460167 c5ar1_human Human No 6.1 IC50 = 877 nM Funct
Antagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrateAntagonist activity at C5a receptor assessed as inhibition of C5a-induced elastase release in human neutrophils during degranulation preincubated 5 mins prior to C5a challenge using p-nitroanilide as substrate
458 4 0 4 6.8 Clc1ccc(Cc2cnc(-c3cccc4ccccc34)n2C2CCC3(CC2)OCCO3)cc1
CHEMBL259645 c5ar1_human Human No 6.1 IC50 = 880 nM Funct
Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilizationAntagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization
444 5 0 3 6.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2ccc(F)cc2C1
CHEMBL471018 c5ar1_human Human No 7.1 IC50 = 89 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
485 6 0 6 5.5 COC(=O)C(CC1CCCCC1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2
CHEMBL3646919 c5ar1_human Human No 8.1 IC50 = 9 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
523 5 1 5 6.8 CO[C@H]1CCN(c2nc(-c3cccc4[nH]cc(C)c34)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)C[C@@H]1C
CHEMBL3646949 c5ar1_human Human No 8.1 IC50 = 9 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
526 5 0 5 7.3 CO[C@@H]1CCN(c2nc(-c3c(C)cc(C)cc3C)nc3c2CN(c2cc(C(C)C)ccc2C)CC3)CC1(C)C
CHEMBL3646982 c5ar1_human Human No 8.1 IC50 = 9 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
441 4 1 5 5.6 COc1nc(-c2c(C)ccc3[nH]nc(C)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL3647030 c5ar1_human Human No 8.1 IC50 = 9 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
546 5 1 8 5.2 CCn1nc(C2CC2)c(Cl)c1N1CCc2nc(-c3c(C)ccc4[nH]nc(C)c34)nc(N3CCOC[C@H]3C)c2C1
CHEMBL334290 c5ar1_human Human No 7.1 IC50 = 90 nM Bind
50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL460167 c5ar1_human Human No 7.1 IC50 = 90 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
458 4 0 4 6.8 Clc1ccc(Cc2cnc(-c3cccc4ccccc34)n2C2CCC3(CC2)OCCO3)cc1
CHEMBL514743 c5ar1_human Human No 7.1 IC50 = 90 nM Bind
Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay
478 4 0 5 7.2 Cc1nc(-c2csc3ccccc23)n(C2CCC3(CC2)OCCO3)c1Cc1ccc(Cl)cc1
CHEMBL469527 c5ar1_human Human No 7.1 IC50 = 90 nM Bind
Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells
483 5 0 4 6.7 CC(C)(CN(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2)c1ccc(Cl)cc1
CHEMBL3646902 c5ar1_human Human No 7.1 IC50 = 90 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
444 3 0 6 5.0 Cc1cc(N2CCc3nc(-c4c(C)cccc4C)nc(N4CCCC(C)(C)C4)c3C2)n(C)n1
CHEMBL431584 c5ar1_human Human No 6.1 IC50 = 900 nM Bind
Tested for the its ability to compete with [125I]-CO13 [125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for the its ability to compete with [125I]-CO13 [125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations
592 9 4 4 4.0 N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O
CHEMBL172841 c5ar1_human Human No 5.1 IC50 = 9000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
381 8 2 3 5.0 C/N=C(/N)Nc1ccc(OCCC2CCCCC2)c(OCc2ccccc2)c1
CHEMBL172952 c5ar1_human Human No 5.1 IC50 = 9000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
337 5 2 3 4.4 C/N=C(/N)Nc1ccc(OCc2ccccc2)c(-c2cccs2)c1
CHEMBL278884 c5ar1_human Human No 5.1 IC50 = 9000 nM Bind
Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937
361 6 3 3 4.5 CNC(=N)Nc1ccc(OCc2ccccc2)c(-c2cccc(OC)c2)c1
CHEMBL3350733 c5ar1_human Human No 5.1 IC50 = 9000 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3646968 c5ar1_human Human No 7.0 IC50 = 91 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
563 5 2 6 4.5 Cc1c[nH]c2cccc(-c3nc4c(c(N5CCN(CC(N)=O)[C@H](C)C5)n3)CN(c3ccccc3C(F)(F)F)CC4)c12
CHEMBL479767 c5ar1_human Human No 6.0 IC50 = 910 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
400 6 1 3 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1C
CHEMBL3350733 c5ar1_human Human No 5.0 IC50 = 9120.1 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(=O)O
CHEMBL3646912 c5ar1_human Human No 7.0 IC50 = 94 nM Funct
FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.FLIPR Assay: Compounds were tested for their ability to inhibit C5a-mediated calcium mobilization using a stable cell line over expressing the human C5aR & the Galpha 15 protein on the FLIPR (Fluorescent Imaging Plate Reader) Tetra system. Cells were maintained in culture media containing DMEM (Dulbecco's Modified Eagle Medium) with 4.5 g/L glucose, 10% fetal bovine serum, 100 U/mL, 1x non-essential amino acid, and 250 ug/mL G418 (Geneticin). Prior to testing of compounds, cells were plated at 10,000 cells/well in clear bottom 384-well black plate, and incubated overnight at 37C. with 5% CO2. On the day of experiment, culture media was removed, and replaced with assay buffer HBSS (Hanks' Balanced Salt Solution) with 20 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) and 0.1% BSA (bovine serum albumin) BSA containing calcium 5 dye (Molecular Devices) and 2.5 mM probenecid. After 1 hour incubation at 37C., 5% CO2 for 60 min, cells were pre-incubated with compounds for 30 minutes.
425 4 2 4 6.0 CNc1nc(-c2cccc3[nH]cc(C)c23)nc2c1CN(c1cc(C(C)C)ccc1C)CC2
CHEMBL480128 c5ar1_human Human No 6.0 IC50 = 950 nM Funct
Antagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant C5a receptor in U937 cells assessed as inhibition of C5a-induced calcium mobilization by FLIPR assay
464 7 0 4 7.1 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cc(OC)ccc1Cl
CHEMBL58781 c5ar1_human Human No 5.0 IC50 = 9500 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL58781 c5ar1_human Human No 5.0 IC50 = 9549.9 nM Bind
Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor
None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CNC(=O)[C@@H](CCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O
CHEMBL481482 c5ar1_human Human No 8.0 Ki = 10 nM Bind
Displacement of [125I]C5a from human recombinant C5a receptor in U937 cellsDisplacement of [125I]C5a from human recombinant C5a receptor in U937 cells
430 7 1 4 6.7 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1cc(OC)ccc1C
CHEMBL3350717 c5ar1_human Human No 5.0 Ki = 10000 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL413040 c5ar1_human Human No 4.0 Ki = 100000 nM Bind
Compound was tested for the inhibition of [125I]C5a binding to C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.Compound was tested for the inhibition of [125I]C5a binding to C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.
None None None CC[C@H](C)[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL429238 c5ar1_human Human No 4.0 Ki = 100000 nM Bind
Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.
None None None None
CHEMBL438915 c5ar1_human Human No 4.0 Ki = 100000 nM Bind
Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCSC)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCSC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O)[C@@H](C)CC)C(C)C)C(C)C)[C@@H](C)O
CHEMBL259984 c5ar1_human Human No 5.9 Ki = 1200 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
468 7 0 5 6.8 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3c(OC)cccc3OC)cc(OC)c21
CHEMBL479395 c5ar1_human Human No 7.9 Ki = 13 nM Bind
Displacement of [125I]C5a from human recombinant C5a receptor in U937 cellsDisplacement of [125I]C5a from human recombinant C5a receptor in U937 cells
450 7 2 4 6.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccc(Cl)cc1CO
CHEMBL339127 c5ar1_human Human No 4.9 Ki = 13000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](N)CC1CCCCC1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL4250011 c5ar1_human Human Yes 7.8 Ki = 15.2 nM Funct
Antagonist activity at recombinant human C5aR1 expressed in Sf9 insect cell membranes co-expressing G-alphai2,G-beta1 and G-gamma2 assessed as inhibition of recombinant human C5a-induced [35S]GTPgammaS binding after 60 mins by liquid scintillation spectrometryAntagonist activity at recombinant human C5aR1 expressed in Sf9 insect cell membranes co-expressing G-alphai2,G-beta1 and G-gamma2 assessed as inhibition of recombinant human C5a-induced [35S]GTPgammaS binding after 60 mins by liquid scintillation spectrometry
554 6 0 2 7.5 C[C@H](N1CCc2c([C@@H]1c1cccc3c1cccc3)cccc2)C(=O)N(C1Cc2c(C1)cccc2)Cc1ccccc1F
CHEMBL3350366 c5ar1_human Human No 5.8 Ki = 1600 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C
CHEMBL260176 c5ar1_human Human No 6.8 Ki = 180 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
480 8 1 4 6.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CCO)c1cccc2ccccc12
CHEMBL410032 c5ar1_human Human No 6.8 Ki = 180 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
468 6 0 2 8.6 CCc1cccc(CC)c1-c1cc(Cl)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL2370691 c5ar1_human Human No 6.7 Ki = 200 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccccc1)C(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL3350715 c5ar1_human Human No 5.7 Ki = 2000 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL128360 c5ar1_human Human No 4.7 Ki = 20000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](C)Nc1nccs1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL480723 c5ar1_human Human No 7.7 Ki = 21 nM Bind
Displacement of [125I]C5a from human recombinant C5a receptor in U937 cellsDisplacement of [125I]C5a from human recombinant C5a receptor in U937 cells
430 8 2 4 5.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2Nc1ccccc1CCO
CHEMBL127385 c5ar1_human Human No 5.7 Ki = 2100 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](N)Cc1cccs1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL408929 c5ar1_human Human No 6.7 Ki = 220 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None None
CHEMBL2369493 c5ar1_human Human No 4.6 Ki = 25000 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL132959 c5ar1_human Human No 6.6 Ki = 260 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None None
CHEMBL3350718 c5ar1_human Human No 5.5 Ki = 2900 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL61726 c5ar1_human Human No 3.5 Ki = 300000 nM Bind
Inhibition of [125I]C5a binding to C5a anaphylatoxin chemotactic receptor in PMNL membranesInhibition of [125I]C5a binding to C5a anaphylatoxin chemotactic receptor in PMNL membranes
None None None None
CHEMBL408493 c5ar1_human Human No 4.5 Ki = 31000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](N)c1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL258658 c5ar1_human Human No 7.5 Ki = 35 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
426 5 0 3 6.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2ccccc2C1
CHEMBL217002 c5ar1_human Human No 4.4 Ki = 36000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL408458 c5ar1_human Human No 6.4 Ki = 370 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
458 5 0 3 8.0 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3cccc4ccccc34)cc(OC)c21
CHEMBL260175 c5ar1_human Human No 5.4 Ki = 3700 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
426 5 0 3 7.0 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3ccccc3F)cc(OC)c21
CHEMBL441393 c5ar1_human Human No 6.4 Ki = 390 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None None
CHEMBL435002 c5ar1_human Human No 5.4 Ki = 4400 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
978 35 13 13 -2.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)CCc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL414570 c5ar1_human Human No 4.3 Ki = 50000 nM Bind
Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.Inhibition of [125I]-C5a anaphylatoxin chemotactic receptor binding to PMNL membranes.
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(C)=O)C(C)C)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL3350714 c5ar1_human Human No 5.3 Ki = 5300 nM Bind
Ability to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptorAbility to inhibit the binding of [125I]C5a anaphylatoxin chemotactic receptor to polymorphonuclear leukocyte (PMNL) membrane receptor
None None None CCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL336081 c5ar1_human Human No 4.2 Ki = 58000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC1=CN(C)CN1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL410927 c5ar1_human Human No 6.2 Ki = 680 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
400 6 0 3 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccccc1
CHEMBL410927 c5ar1_human Human No 6.2 Ki = 680 nM Bind
Displacement of [125I]C5a from human recombinant C5a receptor in U937 cellsDisplacement of [125I]C5a from human recombinant C5a receptor in U937 cells
400 6 0 3 6.4 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1ccccc1
CHEMBL259563 c5ar1_human Human No 8.1 Ki = 7.3 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
450 6 0 3 7.5 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(C)c1cccc2ccccc12
CHEMBL435810 c5ar1_human Human No 4.1 Ki = 79000 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O
CHEMBL259769 c5ar1_human Human No 8.1 Ki = 8.9 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
464 7 0 3 7.9 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL439468 c5ar1_human Human No 6.1 Ki = 810 nM Bind
Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranesInhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes
None None None None
CHEMBL259639 c5ar1_human Human No 5.1 Ki = 8300 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
408 5 0 3 6.8 CCN(c1cccc2ccccc12)C1CCCc2nc(-c3ccccc3)cc(OC)c21
CHEMBL259643 c5ar1_human Human No 7.1 Ki = 86 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
436 6 0 3 7.4 CCc1ccccc1-c1cc(OC)c2c(n1)CCCC2N(CC)c1cccc2ccccc12
CHEMBL262330 c5ar1_human Human No 8.0 Ki = 9.7 nM Bind
Displacement of [125I]C5a from human C5a receptor in U937 cellsDisplacement of [125I]C5a from human C5a receptor in U937 cells
494 5 0 3 7.3 CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N1CCc2cccc(C(F)(F)F)c2C1