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ChEMBL ligand: CHEMBL518924 (Amd 070, AMD-070, AMD070, AMD-11070, AMD11070, 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] | ||||||||
ChEMBL | Binding affinity to CXCR4 (unknown origin) assessed as inhibition constant | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2017) 60: 4735-4779 [PMID:28165741] |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]