Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T06955 | Target Info | |||
| Target Name | C-C chemokine receptor type 4 (CCR4) | ||||
| Synonyms |
K5-5; CMKBR4; CD194; CCR-4; CC-CKR-4; CC chemokine receptor 4; C-CCKR-4; C-C CKR-4
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| Target Type | Successful Target | ||||
| Gene Name | CCR4 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Flavonoid derivative 4
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|
Patented | Compound Info | ||
| Synonyms |
PMID26394986-Compound-48
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
11-Butyl-3-[1-(4,6-dimethylpyrimidine-5-carbonyl)-4-methyl-4-piperidyl]-9-[(4-ethoxycyclohexyl)methyl]-3,9-diazaspiro[5.5]undecan-10-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL449621; SCHEMBL3963928; BDBM50254750
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
PharmaGSID_48521
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1078231; DSSTox_CID_28495; DSSTox_RID_82770; DSSTox_GSID_48521; DTXSID8048521; SCHEMBL18841093; Tox21_303454; BDBM50310739; NCGC00257432-01
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-(4-(4-Fluorophenyl)piperazin-1-yl)-5,7-dihydroxy-4-methyl-2H-chromen-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL602269; BDBM50307039; 3-[4-(4-fluorophenyl)piperazin-1-yl]-5,7-dihydroxy-4-methylchromen-2-one
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| Activity |
IC50 = 58500 nM
|
[4] | |||
| Compound Name |
N-(3-Morpholin-4-yl-propyl)-2-((1R,4R)-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-2-thiophen-3-yl-thiazolidin-3-yl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL42360; BDBM50142351
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|
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| Activity |
IC50 = 66000 nM
|
[5] | |||
| Compound Name |
2-((1R,4R)-2-Furan-3-yl-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL44463; BDBM50142417
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| Activity |
IC50 = 100000 nM
|
[5] | |||
| Compound Name |
2-((1R,4R)-2-(2,4-Bis-trifluoromethyl-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL298193; BDBM50142400
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-((1R,4R)-2-Cyclohexyl-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL416069; BDBM50142386
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| Activity |
IC50 = 100000 nM
|
[5] | |||
| Compound Name |
2-((1R,4R)-2-Benzyl-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL297761; BDBM50142396
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-[(2R,5R)-2-(2,4-Dichloro-phenyl)-3-(3-morpholin-4-ylmethyl-benzyl)-4-oxo-thiazolidin-5-yl]-N-naphthalen-1-ylmethyl-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL43330; BDBM50142374
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|
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| Activity |
IC50 = 100000 nM
|
[5] | |||
| Compound Name |
N-(3-Morpholin-4-yl-propyl)-2-((1R,4R)-5-{[(naphthalen-1-ylmethyl)-carbamoyl]-methyl}-4-oxo-2-phenethyl-thiazolidin-3-yl)-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL296245; BDBM50142360
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|
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| Activity |
IC50 = 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Amino-N-((2S,3R)-1-(2,6-dioxopiperidin-3-ylamino)-3-methyl-1-oxopentan-2-yl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL605999; BDBM50307057
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| Activity |
IC50 = 836000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Colloidal aggregation causes inhibition of G protein-coupled receptors. J Med Chem. 2013 Mar 28;56(6):2406-14. | ||||
| REF 2 | Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist. Bioorg Med Chem Lett. 2009 Jan 1;19(1):209-13. | ||||
| REF 3 | Spiropiperidine CCR5 antagonists. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5401-6. | ||||
| REF 4 | Discovery and optimization of novel 3-piperazinylcoumarin antagonist of chemokine-like factor 1 with oral antiasthma activity in mice. J Med Chem. 2010 Feb 25;53(4):1741-54. | ||||
| REF 5 | Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1619-24. | ||||
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