General Information of the Protein
Protein ID
PT04108
Protein Name
Atypical chemokine receptor 3
Secondarily
Protein Name
C-X-C chemokine receptor type 7
Chemokine orphan receptor 1
G-protein coupled receptor 159
G-protein coupled receptor RDC1 homolog
Gene Name
ACKR3
Secondarily
Gene Name
CMKOR1
CXCR7
GPR159
RDC1
Sequence
MDLHLFDYSEPGNFSDISWPCNSSDCIVVDTVMCPNMPNKSVLLYTLSFIYIFIFVIGMIANSVVVWVNIQAKTTGYDTHCYILNLAIADLWVVLTIPVWVVSLVQHNQWPMGELTCKVTHLIFSINLFGSIFFLTCMSVDRYLSITYFTNTPSSRKKMVRRVVCILVWLLAFCVSLPDTYYLKTVTSASNNETYCRSFYPEHSIKEWLIGMELVSVVLGFAVPFSIIAVFYFLLARAISASSDQEKHSSRKIIFSYVVVFLVCWLPYHVAVLLDIFSILHYIPFTCRLEHALFTALHVTQCLSLVHCCVNPVLYSFINRNYRYELMKAFIFKYSAKTGLTKLIDASRVSETEYSALEQSTK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Chemokine receptor
>
CXC chemokine receptor
Function
Atypical chemokine receptor that controls chemokine levels and localization via high-affinity chemokine binding that is uncoupled from classic ligand-driven signal transduction cascades, resulting instead in chemokine sequestration, degradation, or transcytosis. Also known as interceptor (internalizing receptor) or chemokine-scavenging receptor or chemokine decoy receptor. Acts as a receptor for chemokines CXCL11 and CXCL12/SDF1 (PubMed:16107333, PubMed:19255243, PubMed:19380869, PubMed:20161793, PubMed:22300987). Chemokine binding does not activate G-protein-mediated signal transduction but instead induces beta-arrestin recruitment, leading to ligand internalization and activation of MAPK signaling pathway (PubMed:16940167, PubMed:18653785, PubMed:20018651). Required for regulation of CXCR4 protein levels in migrating interneurons, thereby adapting their chemokine responsiveness (PubMed:16940167, PubMed:18653785). In glioma cells, transduces signals via MEK/ERK pathway, mediating resistance to apoptosis. Promotes cell growth and survival (PubMed:16940167, PubMed:20388803). Not involved in cell migration, adhesion or proliferation of normal hematopoietic progenitors but activated by CXCL11 in malignant hemapoietic cells, leading to phosphorylation of ERK1/2 (MAPK3/MAPK1) and enhanced cell adhesion and migration (PubMed:17804806, PubMed:18653785, PubMed:19641136, PubMed:20887389). Plays a regulatory role in CXCR4-mediated activation of cell surface integrins by CXCL12 (PubMed:18653785). Required for heart valve development (PubMed:17804806). Regulates axon guidance in the oculomotor system through the regulation of CXCL12 levels (PubMed:31211835).
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Uniprot ID
Primary ID:
P25106

Secondarily ID:
A8K6J4
Q53RV4
Q8NE10
Q92938
Q92986
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Ensembl ID
ENSG00000144476
HGNC ID
HGNC:23692
Subcellular Location
Cell membrane
Early endosome
Recycling endosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0389144
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-8-(naphthalen-1-ylmethyl)-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C49H58N10O7
 1
1
IC50 = 170 nM
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CP0472888
3-[(1S,4R,7S,10S,13S)-7-[3-(diaminomethylideneamino)propyl]-4-[(4-hydroxyphenyl)methyl]-9-methyl-13-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-3,6,9,12,15-pentazatricyclo[13.7.0.016,21]docosa-16,18,20-trien-10-yl]propylurea
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C44H52N10O7
 1
1
IC50 = 190 nM
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CP0521749
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-9-(sulfanylmethyl)-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C37H46N8O6S
 1
1
IC50 = 250 nM
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CP0475176
3-[(1S,4R,7S,10S,13S,16S,21S)-7-[3-(diaminomethylideneamino)propyl]-4-[(4-hydroxyphenyl)methyl]-9-methyl-13-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-3,6,9,12,15-pentazatricyclo[13.7.0.016,21]docosan-10-yl]propylurea
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C44H58N10O7
 1
1
IC50 = 350 nM
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CP0472743
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(2-fluorophenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51FN10O6
 1
1
IC50 = 410 nM
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CP0471609
2-[4-[(2S,5S,8S,11S,14R)-5-[4-(diaminomethylideneamino)butyl]-14-[(2-fluorophenyl)methyl]-4,10-dimethyl-11-(naphthalen-1-ylmethyl)-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]butyl]guanidine
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C51H62FN11O5
 1
1
IC50 = 450 nM
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CP0472891
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C47H57N11O7
 1
1
IC50 = 520 nM
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CP0521751
3-[(3S,6S,9S,12R,15S)-12-(1-benzothiophen-3-ylmethyl)-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C42H52N10O6S
 1
1
IC50 = 540 nM
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CP0468869
2-[3-[(3S,6S,9S,12R,15S)-6-[4-(diaminomethylideneamino)butyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C41H55N11O6
 1
1
IC50 = 560 nM
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CP0470852
3-[(2S,5S,8S,11R,14S)-8-benzyl-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C45H56N10O7
 1
1
IC50 = 600 nM
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CP0468870
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3,12-bis(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C44H54N10O6
 1
1
IC50 = 690 nM
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CP0471605
3-[(3S,6S,9S,12R,15S)-12-[(4-bromophenyl)methyl]-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51BrN10O6
 1
1
IC50 = 720 nM
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CP0471606
3-[(3S,6S,9S,12R,15S)-12-[(4-benzoylphenyl)methyl]-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C47H56N10O7
 1
1
IC50 = 720 nM
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CP0468863
3-[(3S,6S,9S,12R,15S)-12-[(4-chlorophenyl)methyl]-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51ClN10O6
 1
1
IC50 = 790 nM
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CP0385437
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C40H53N11O6
 2
1
IC50 = 800 nM
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2
IC50 = 860 nM
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CP0432165
2-[3-[(3S,6S,9S,12R,15S)-9-[4-(diaminomethylideneamino)butyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C41H55N11O6
 1
1
IC50 = 840 nM
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CP0471607
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-1-methyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C46H55N11O7
 1
1
IC50 = 850 nM
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CP0389145
3-[(2S,5S,8S,11R,14S)-8-(1-benzothiophen-3-ylmethyl)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C47H56N10O7S
 1
1
IC50 = 1000 nM
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CP0483104
3-[(3S,6S,9S,12R,15S)-12-benzyl-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H52N10O6
 1
1
IC50 = 1100 nM
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CP0472885
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(4-fluorophenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51FN10O6
 1
1
IC50 = 1200 nM
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CP0477926
7-[2-hydroxy-3-(3-methylpiperidin-1-yl)propoxy]-2,3-dihydro-1H-cyclopenta[c]chromen-4-one
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C21H27NO4
 1
1
IC50 = 1290 nM
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CP0396368
2-[3-[(3S,6S,9S,12R,15S)-6-(3-aminopropyl)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C39H51N9O6
 1
1
IC50 = 1300 nM
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CP0513911
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(3-fluorophenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51FN10O6
 1
1
IC50 = 1300 nM
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CP0410002
N-(1-benzylpiperidin-4-yl)-2-(4,7-dimethyl-2-oxochromen-5-yl)oxyacetamide
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C25H28N2O4
 1
1
IC50 = 1490 nM
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CP0376673
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C39H51N11O6
 1
1
IC50 = 1500 nM
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CP0560428
2-[3-[(3S,6S,9S,12R,15S)-6-[2-(diaminomethylideneamino)ethyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C39H51N11O6
 1
1
IC50 = 1500 nM
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CP0444549
2-[3-[(3S,6S,9R,12S,15S,18R)-12-[(2S)-butan-2-yl]-6-[3-(diaminomethylideneamino)propyl]-15-[(1R)-1-hydroxyethyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-9-yl]propyl]guanidine
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C40H60N12O7
 1
1
IC50 = 1700 nM
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CP0471610
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-8-(2-methylsulfanylethyl)-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C41H56N10O7S
 1
1
IC50 = 1800 nM
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CP0519963
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-8,11-bis[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C45H56N10O8
 1
1
IC50 = 1800 nM
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CP0527579
5-(4-bromophenyl)-N-[2-(2-methoxyphenyl)-2-(4-methylpiperidin-1-yl)ethyl]-1,2-oxazole-3-carboxamide
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C25H28BrN3O3
 1
1
IC50 = 1870 nM
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CP0417680
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-8-(2-methylpropyl)-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
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C42H58N10O7
 1
1
IC50 = 1900 nM
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CP0389191
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-7-methyl-9-(2-methylpropyl)-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C40H52N8O6
 1
1
IC50 = 2000 nM
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CP0396371
2-[3-[(3S,6S,9S,12R,15S)-9-(hydroxymethyl)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C37H46N8O7
 1
1
IC50 = 2000 nM
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CP0468864
2-[3-[(3S,6S,9S,12R,15S)-9-[(1R)-1-hydroxyethyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C38H48N8O7
 1
1
IC50 = 2000 nM
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CP0470853
2-[3-[(3R,6S,12S,15S,18S)-3-[(4-hydroxyphenyl)methyl]-16-methyl-12-(naphthalen-2-ylmethyl)-2,5,11,14,17-pentaoxo-1,4,10,13,16-pentazatricyclo[16.3.0.06,10]henicosan-15-yl]propyl]guanidine
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C39H48N8O6
 1
1
IC50 = 2000 nM
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CP0470854
2-[3-[(3S,6S,9S,12R,15S)-9,12-bis[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C43H50N8O7
 1
1
IC50 = 2000 nM
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CP0470860
2-[3-[(3S,6S,9S,12R,15S)-9-(4-aminobutyl)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C40H53N9O6
 1
1
IC50 = 2000 nM
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CP0471608
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-9-(1H-indol-3-ylmethyl)-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C45H51N9O6
 1
1
IC50 = 2000 nM
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CP0471611
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-9-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C39H50N8O6
 1
1
IC50 = 2000 nM
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CP0475178
2-[3-[(3S,6S,9S,12R,15S)-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C40H52N8O6
 1
1
IC50 = 2000 nM
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CP0475179
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-7-methyl-9-(2-methylsulfanylethyl)-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C39H50N8O6S
 1
1
IC50 = 2000 nM
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CP0475180
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-9-(1H-imidazol-5-ylmethyl)-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C40H48N10O6
 1
1
IC50 = 2000 nM
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CP0513909
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-12-[(4-nitrophenyl)methyl]-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
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C40H51N11O8
 1
1
IC50 = 2000 nM
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CP0538841
2-[3-[(3S,6S,9S,12R,15S)-9-benzyl-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
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C43H50N8O6
 1
1
IC50 = 2000 nM
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CP0521744
3-[(1S,4R,7S,10S,13S)-7-[3-(diaminomethylideneamino)propyl]-4-[(4-hydroxyphenyl)methyl]-9-methyl-13-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-3,6,9,12,15,24-hexazatetracyclo[13.11.0.017,25.018,23]hexacosa-17(25),18,20,22-tetraen-10-yl]propylurea
   Show/Hide
C47H55N11O7
 1
1
IC50 = 2100 nM
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CP0397532
2-(6-chloro-1-methyl-2-oxoquinolin-4-yl)sulfanyl-N-[3-(2-ethylpiperidin-1-yl)propyl]acetamide
   Show/Hide
C22H30ClN3O2S
 1
1
IC50 = 2160 nM
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CP0417679
3-[(2S,5S,8S,11R,14S)-8-[(2S)-butan-2-yl]-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
   Show/Hide
C42H58N10O7
 1
1
IC50 = 2200 nM
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CP0380467
N-[3-[benzyl(methyl)amino]propyl]-5-methyl-4-oxothieno[3,2-c]quinoline-2-carboxamide
   Show/Hide
C24H25N3O2S
 1
1
IC50 = 2210 nM
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CP0406995
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-10-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 2400 nM
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CP0513910
2-[3-[(3S,6S,9S,12R,15S)-9-[2-(diaminomethylideneamino)ethyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
   Show/Hide
C39H51N11O6
 1
1
IC50 = 2600 nM
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CP0513914
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5,8-bis(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
   Show/Hide
C49H58N10O7
 1
1
IC50 = 2600 nM
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CP0573798
2-[3-[(3S,6S,9S,12R,15S)-9-(3-aminopropyl)-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
   Show/Hide
C39H51N9O6
 1
1
IC50 = 2600 nM
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CP0563096
8-methyl-N-[2-(2-methylpiperidin-1-yl)ethyl]-4H-chromeno[3,4-d][1,2]oxazole-3-carboxamide
   Show/Hide
C20H25N3O3
 1
1
IC50 = 2640 nM
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CP0397475
N-[3-[benzyl(ethyl)amino]propyl]-2-(4-methyl-1-oxo-[1]benzothiolo[2,3-d]pyridazin-2-yl)butanamide
   Show/Hide
C27H32N4O2S
 1
1
IC50 = 2780 nM
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CP0563095
N-[3-(3,5-dimethylpiperidin-1-yl)propyl]-8-methyl-4H-chromeno[3,4-d][1,2]oxazole-3-carboxamide
   Show/Hide
C22H29N3O3
 1
1
IC50 = 2920 nM
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CP0381272
[5-(2,3-dihydroindol-1-yl)thiophen-2-yl]-(4-piperidin-1-ylpiperidin-1-yl)methanone
   Show/Hide
C23H29N3OS
 1
1
IC50 = 3200 nM
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CP0389146
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
   Show/Hide
C42H53N11O6
 1
1
IC50 = 3200 nM
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CP0446853
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-4-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 3400 nM
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CP0389244
3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propylurea
   Show/Hide
C40H52N10O7
 1
1
IC50 = 3600 nM
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CP0477925
N-[2-[butyl(ethyl)amino]ethyl]-5-(2,3-dihydroindol-1-yl)thiophene-2-carboxamide
   Show/Hide
C21H29N3OS
 1
1
IC50 = 3890 nM
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CP0475177
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-8-[(4-phenylphenyl)methyl]-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
   Show/Hide
C51H60N10O7
 1
1
IC50 = 4000 nM
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CP0560501
2-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]acetamide
   Show/Hide
C38H47N9O7
 1
1
IC50 = 4100 nM
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CP0519962
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazatricyclo[13.8.0.017,22]tricosa-17,19,21-trien-6-yl]propylurea
   Show/Hide
C45H54N10O7
 1
1
IC50 = 4200 nM
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CP0540612
4-methyl-N-[5-[(3-phenylpyrrolidin-1-yl)methyl]-1,3-thiazol-2-yl]benzamide
   Show/Hide
C22H23N3OS
 1
1
IC50 = 4350 nM
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CP0431334
2-[3-[(3S,6R,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 4600 nM
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CP0432529
2-[3-[(3S,6S,9R,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C39H51N11O6
 1
1
IC50 = 4600 nM
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CP0417678
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-8-(sulfanylmethyl)-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
   Show/Hide
C39H52N10O7S
 1
1
IC50 = 4600 nM
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CP0472889
3-[(2S,5S,8S,11R,14S)-14-[3-(diaminomethylideneamino)propyl]-11-[(4-hydroxyphenyl)methyl]-1,7-dimethyl-5-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]propylurea
   Show/Hide
C41H56N10O7
 1
1
IC50 = 4900 nM
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CP0389188
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-12-(2-phenylethyl)-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
   Show/Hide
C41H54N10O6
 1
1
IC50 = 5000 nM
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CP0482405
7-chloro-N-[2-(2-methylpiperidin-1-yl)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide
   Show/Hide
C20H23ClN2OS2
 1
1
IC50 = 5270 nM
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CP0540611
(5Z)-5-[[4-(dimethylamino)phenyl]methylidene]-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4-one
   Show/Hide
C18H24N4O2S
 1
1
IC50 = 5360 nM
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CP0463442
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propanamide
   Show/Hide
C39H49N9O7
 1
1
IC50 = 5800 nM
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CP0482404
(E)-N-[2-[[cyclohexyl(methyl)amino]methyl]phenyl]-3-(1-phenylpyrazol-4-yl)prop-2-enamide
   Show/Hide
C26H30N4O
 1
1
IC50 = 5840 nM
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CP0381271
N-[(1-ethylpyrrolidin-2-yl)methyl]-2-[(2Z)-2-[(2-fluorophenyl)methylidene]-3-oxo-1,4-benzothiazin-4-yl]acetamide
   Show/Hide
C24H26FN3O2S
 1
1
IC50 = 6190 nM
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CP0399441
N-[(1-ethylpyrrolidin-2-yl)methyl]-5-indol-1-ylthiophene-2-carboxamide
   Show/Hide
C20H23N3OS
 1
1
IC50 = 6750 nM
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CP0477924
N-[2-(azepan-1-yl)ethyl]-8-methyl-4-oxo-5H-thieno[3,2-c]quinoline-2-carboxamide
   Show/Hide
C21H25N3O2S
 1
1
IC50 = 7000 nM
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CP0381270
7-[2-hydroxy-3-(2-methylpiperidin-1-yl)propoxy]-2,3-dihydro-1H-cyclopenta[c]chromen-4-one
   Show/Hide
C21H27NO4
 1
1
IC50 = 8020 nM
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CP0460508
3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propanamide
   Show/Hide
C39H49N9O7
 1
1
IC50 = 9500 nM
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CP0433064
N-[4-[3-(dimethylamino)propylcarbamothioylamino]-2,5-diethoxyphenyl]-4-methylbenzamide
   Show/Hide
C24H34N4O3S
 1
1
IC50 = 9790 nM
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CP0365172
(3-amino-6-ethyl-7,8-dihydro-5H-thieno[2,3-b][1,6]naphthyridin-2-yl)-(3,4-dihydro-1H-isoquinolin-2-yl)methanone
   Show/Hide
C22H24N4OS
 1
1
IC50 = 10000 nM
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CP0395374
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-6,7-dimethyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C37H46N8O6
 1
1
IC50 = 11000 nM
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CP0380465
N-[3-[cyclopentyl(furan-2-ylmethyl)amino]propyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide
   Show/Hide
C25H28N2O2S2
 1
1
IC50 = 11400 nM
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CP0446855
2-[3-[(3S,6S,9R,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-10-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 13000 nM
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CP0510917
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.4.0]nonadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 13000 nM
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CP0521750
3-[(3S,6S,9S,12R,15S)-9-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-7-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propylurea
   Show/Hide
C40H52N10O7
 1
1
IC50 = 13000 nM
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CP0388842
2-[3-[(2S,5S,8S,11S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-10,11-dimethyl-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
   Show/Hide
C38H51N11O6
 1
1
IC50 = 15000 nM
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CP0406996
2-[3-[(3S,6S,9S,12R,15S)-12-[(4-hydroxyphenyl)methyl]-7,9-dimethyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-6-yl]propyl]guanidine
   Show/Hide
C37H46N8O6
 1
1
IC50 = 16000 nM
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CP0446854
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-13-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 18000 nM
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CP0510916
2-[3-[(2S,5S,8S,11S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-11-methyl-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
   Show/Hide
C37H49N11O6
 1
1
IC50 = 18000 nM
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CP0432531
2-[3-[(3S,6S,9S,12S,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-13-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 = 23000 nM
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CP0248152
2-[3-[(2S,5S,8S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
   Show/Hide
C36H47N11O6
 1
1
IC50 > 30000 nM
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CP0388841
2-[3-[(2S,5S,8S,11R,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-11-methyl-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
   Show/Hide
C37H49N11O6
 1
1
IC50 > 30000 nM
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CP0388907
2-[3-[(3S,6S,9S,12S,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C39H51N11O6
 1
1
IC50 > 30000 nM
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CP0431330
2-[3-[(3R,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-4-methyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C40H53N11O6
 1
1
IC50 > 30000 nM
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CP0431331
2-[3-[(2R,5S,8S,11S)-8-[3-(diaminomethylideneamino)propyl]-2-[(4-hydroxyphenyl)methyl]-11-(naphthalen-2-ylmethyl)-3,6,9,12,16-pentaoxo-1,4,7,10,13-pentazacyclohexadec-5-yl]propyl]guanidine
   Show/Hide
C37H49N11O6
 1
1
IC50 > 30000 nM
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CP0431332
2-[3-[(3S,6S,9S,12R,15R)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C39H51N11O6
 1
1
IC50 > 30000 nM
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CP0431333
2-[3-[(3R,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C39H51N11O6
 1
1
IC50 > 30000 nM
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CP0431335
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-7,12-dimethyl-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
   Show/Hide
C34H49N11O5
 1
1
IC50 > 30000 nM
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CP0432534
2-[3-[(3S,6S,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3,7-dimethyl-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C30H47N11O6
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0432577
2-[3-[(2S,5S,8S,11R,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-10,11-dimethyl-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine
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C38H51N11O6
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0504621
2-[3-[(3S,6S,9S,12R,15R)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.4.0]nonadecan-9-yl]propyl]guanidine
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C40H53N11O6
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0510918
2-[3-[(3S,6R,9S,12R,15S)-6-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-3-(naphthalen-2-ylmethyl)-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-9-yl]propyl]guanidine
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C39H51N11O6
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0236196
[4-[[4-(7-ethylimidazo[1,2-a]pyridin-8-yl)-1,4-diazepan-1-yl]methyl]piperidin-1-yl]-[(1R,2S,4S)-7-oxabicyclo[2.2.1]heptan-2-yl]methanone
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C27H39N5O2
 1
1 Ki = 47 nM
Clinical Information about the Protein
Target 1 ( C-X-C chemokine receptor type 7 (ACKR3) )
Target Type Preclinical Target
Disease 1 Target-related Disease  1
1 Asthma [ICD-11: CA23]
Discontinued Drug(s) 1 Discontinued Drug  1
1 GW-766994 Discontinued in Phase 2
Asthma
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT07742 Atypical chemokine receptor 3 Canis lupus familiaris, Dog, Canis familiaris