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ChEMBL ligand: CHEMBL518924 (Amd070, Amd 070, AMD070, AMD-070, AMD11070, AMD-11070, Cxcr4 inhibitor x4p-001, Mavorixafor, X4p001, X 4P-001, X4P-001) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | Inhibition of alpha 2A adrenergic receptor (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246] | ||||||||
ChEMBL | Displacement of radiolabeled MIP1alpha from CCR1 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597] | ||||||||
ChEMBL | Displacement of radiolabeled MCP1 from CCR2b receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
CCR4/C-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679] | ||||||||
ChEMBL | Displacement of radiolabeled TARC from CCR4 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
ChEMBL | Displacement of radiolabeled MIP1beta from CCR5 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
CXCR4/C-X-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073] | ||||||||
GtoPdb | Assay using 125I-SDF-1α as tracer, in Cf2Th cells expressing hCXCR4. | - | 7.96 | pKi | 11 | nM | Ki | Mol Pharmacol (2008) 74: 1485-95 [PMID:18768385] |
ChEMBL | Antagonist activity at CXCR4 in human PBMC assessed as inhibition of HIV-1 3B infection | B | 7.52 | pIC50 | 30 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1025-1030 [PMID:24936240] |
ChEMBL | Displacement of [125I]SDF-1-alpha from CXCR4 in human CEM-CCRF cells by liquid scintillation counting | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
GtoPdb | Displacement of [125I]SDF-1α binding from CXCR4 in human CEM-CCRF cells by liquid scintillation counting. | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2010) 53: 3376-88 [PMID:20297846] |
ChEMBL | Antagonist activity at CXCR4 receptor in human CCRF-CEM cells assessed as inhibition of SDF-1alpha-induced calcium release preincubated for 25 mins followed by SDF-1alpha addition and monitered for 90 sec | F | 8.29 | pIC50 | 5.18 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1605-1612 [PMID:34676043] |
ChEMBL | Antagonist activity at CXCR4 in human CCRF-CEM cells assessed as inhibition of SDS1alpha-induced calcium flux pretreated for 25 mins followed by SDS1alpha addition measured for 90 secs by calcium-dye based assay | F | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2018) 9: 446-451 [PMID:29795757] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Inhibition of dopamine D2 receptor (unknown origin) | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024] | ||||||||
ChEMBL | Displacement of radiolabeled IL8 from CXCR1 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025] | ||||||||
ChEMBL | Displacement of radiolabeled IL8 from CXCR2 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3376-3388 [PMID:20297846] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Inhibition of kappa opioid receptor (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Inhibition of mu opioid receptor (unknown origin) | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Inhibition of M2 mAChR receptor (unknown origin) | B | 5.12 | pIC50 | 7500 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
ChEMBL | Inhibition of alpha7 nicotinic acetylcholine receptor (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 4058-4084 [PMID:35179893] |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]