Reaction Details |
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Target | C-C chemokine receptor type 3 |
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Ligand | BDBM50231358 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_465934 (CHEMBL947058) |
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IC50 | 0.04±n/a nM |
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Citation | Santella, JB; Gardner, DS; Yao, W; Shi, C; Reddy, P; Tebben, AJ; DeLucca, GV; Wacker, DA; Watson, PS; Welch, PK; Wadman, EA; Davies, P; Solomon, KA; Graden, DM; Yeleswaram, S; Mandlekar, S; Kariv, I; Decicco, CP; Ko, SS; Carter, PH; Duncia, JV From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis. Bioorg Med Chem Lett18:576-85 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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C-C chemokine receptor type 3 |
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Name: | C-C chemokine receptor type 3 |
Synonyms: | C-C CKR-3 | C-C chemokine receptor type 3 (CCR3) | CC-CKR-3 | CCR-3 | CCR3 | CCR3_HUMAN | CD_antigen=CD193 | CKR3 | CMKBR3 | Eosinophil eotaxin receptor |
Type: | Enzyme |
Mol. Mass.: | 41053.88 |
Organism: | Homo sapiens (Human) |
Description: | P51677 |
Residue: | 355 |
Sequence: | MTTSLDTVETFGTTSYYDDVGLLCEKADTRALMAQFVPPLYSLVFTVGLLGNVVVVMILI
KYRRLRIMTNIYLLNLAISDLLFLVTLPFWIHYVRGHNWVFGHGMCKLLSGFYHTGLYSE
IFFIILLTIDRYLAIVHAVFALRARTVTFGVITSIVTWGLAVLAALPEFIFYETEELFEE
TLCSALYPEDTVYSWRHFHTLRMTIFCLVLPLLVMAICYTGIIKTLLRCPSKKKYKAIRL
IFVIMAVFFIFWTPYNVAILLSSYQSILFGNDCERSKHLDLVMLVTEVIAYSHCCMNPVI
YAFVGERFRKYLRHFFHRHLLMHLGRYIPFLPSEKLERTSSVSPSTAEPELSIVF
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BDBM50231358 |
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n/a |
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Name | BDBM50231358 |
Synonyms: | 1-((2R,3S)-4-((S)-3-(4-fluorobenzyl)piperidin-1-yl)-3-hydroxybutan-2-yl)-3-(3-(1-methyl-1H-tetrazol-5-yl)phenyl)urea | 1-{(1R,2S)-3-[(S)-3-(4-Fluoro-benzyl)-piperidin-1-yl]-2-hydroxy-1-methyl-propyl}-3-[3-(1-methyl-1H-tetrazol-5-yl)-phenyl]-urea | BMS-639623 | CHEMBL399495 |
Type | Small organic molecule |
Emp. Form. | C25H32FN7O2 |
Mol. Mass. | 481.5657 |
SMILES | C[C@@H](NC(=O)Nc1cccc(c1)-c1nnnn1C)[C@@H](O)CN1CCC[C@@H](Cc2ccc(F)cc2)C1 |r| |
Structure |
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