cilengitide [Ligand Id: 6597] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL429876 (Cilengitide, EMD-12192, EMD 121974, EMD-121974) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| integrin, beta 1 subunit (fibronectin receptor, beta polypeptide, antigen CD29 includes MDF2, MSK12)/integrin, alpha 5 subunit (fibronectin receptor, alpha polypeptide)/Integrin alpha-5/beta-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095226] [GtoPdb: 2455, 2444] [UniProtKB: P05556, P08648] | ||||||||
| ChEMBL | Inhibition of fibronectin binding to human alpha5beta1 integrin after 1 hr by ELISA | B | 5 | pIC50 | 10100 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Binding affinity to alpha5beta1 integrin (unknown origin) | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Inhibition of fibronectin binding to human alpha5beta1 integrin receptor after 1 hr by competitive solid-phase binding ELISA | B | 7.81 | pIC50 | 15.4 | nM | IC50 | J Med Chem (2014) 57: 3410-3417 [PMID:24654918] |
| ChEMBL | Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay | B | 7.81 | pIC50 | 15.4 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127039-127039 [PMID:32094009] |
| ChEMBL | Binding affinity to human integrin alpha5beta1 incubated for 1 hr by ELISA based solid phase integrin binding assay | B | 7.81 | pIC50 | 15.4 | nM | IC50 | J Med Chem (2021) 64: 586-601 [PMID:33356253] |
| ChEMBL | Inhibition of fibronectin binding to soluble alpha5beta1 integrin (unknown origin) after 1 hr by ELISA | B | 7.81 | pIC50 | 15.4 | nM | IC50 | J Med Chem (2018) 61: 4791-4809 [PMID:29775303] |
| ChEMBL | Inhibition of human fibronectin binding to human integrin alpha5beta1 incubated for 1 hr by ELISA | B | 7.81 | pIC50 | 15.4 | nM | IC50 | J Med Chem (2019) 62: 7417-7430 [PMID:31306009] |
| ChEMBL | Inhibition of fibronectin binding to human Integrin alpha5beta1 receptor by competitive ELISA | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2013) 56: 1509-1519 [PMID:23362923] |
| ChEMBL | Antagonist activity at alpha5beta1 integrin receptor (unknown origin) by cell-free ELISA | B | 7.88 | pIC50 | 13.2 | nM | IC50 | J Med Chem (2014) 57: 6301-6315 [PMID:24568695] |
| integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)/Integrin alpha-IIb/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2093869] [GtoPdb: 2457, 2441] [UniProtKB: P05106, P08514] | ||||||||
| ChEMBL | Inhibition of fibrinogen binding to Integrin alpha2bbeta3 receptor (unknown origin) by competitive ELISA | B | 5.38 | pIC50 | 4208 | nM | IC50 | J Med Chem (2013) 56: 1509-1519 [PMID:23362923] |
| ChEMBL | Inhibition of fibrinogen binding to alpha2bbeta3 integrin receptor (unknown origin) after 1 hr by competitive solid-phase binding ELISA | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2014) 57: 3410-3417 [PMID:24654918] |
| ChEMBL | Inhibition of fibrinogen binding to recombinant human platelet glycoprotein alpha IIb beta3 integrin | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| integrin, alpha V subunit/integrin, alpha 5 subunit (fibronectin receptor, alpha polypeptide)/Integrin alpha-V/alpha-5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430893] [GtoPdb: 2453, 2444] [UniProtKB: P06756, P08648] | ||||||||
| ChEMBL | Displacement of [125I]echistatin from integrin alphaVbeta5 receptor in human placenta by microplate scintillation counter | B | 9.89 | pIC50 | 0.13 | nM | IC50 | Bioorg Med Chem (2009) 17: 1542-1549 [PMID:19195898] |
| integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/Integrin alpha-V/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907598] [GtoPdb: 2457, 2453] [UniProtKB: P05106, P06756] | ||||||||
| ChEMBL | Binding affinity to human integrin alphaVbeta3 receptor using acetyl-CisoDGRCGVRSSSRTPSDKY-bio probe and streptavidin-peroxidase conjugate incubated for 3 hrs by competitive binding assay | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2018) 61: 7474-7485 [PMID:29883545] |
| ChEMBL | Binding affinity to alphaVbeta3 integrin (unknown origin) | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6 | F | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| ChEMBL | Binding affinity to alphaVbeta3 integrin in human SKOV3 cells assessed as inhibition of cell adhesion to fibrinogen measured after 2 hrs by MTT assay | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 896-900 [PMID:30732943] |
| ChEMBL | Antagonist activity at integrin alphaVbeta3 (unknown origin) expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1911-1913 [PMID:28351594] |
| ChEMBL | Inhibition of vitronectin binding to human alphaVbeta3 integrin after 2 hrs by ELISA | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Displacement of [125I]echistatin from integrin alphaVbeta3 receptor in human placenta by microplate scintillation counter | B | 7.72 | pIC50 | 18.9 | nM | IC50 | Bioorg Med Chem (2009) 17: 1542-1549 [PMID:19195898] |
| ChEMBL | Displacement of [125I]echistatin from AlphaV-beta-3 integrin receptor | B | 7.72 | pIC50 | 18.9 | nM | IC50 | J Med Chem (2006) 49: 1808-1817 [PMID:16509596] |
| ChEMBL | Displacement of [125I]echistatin from human integrin alpha-V-beta-3 receptor by solid phase assay | B | 7.72 | pIC50 | 18.9 | nM | IC50 | J Med Chem (2008) 51: 1771-1782 [PMID:18303826] |
| ChEMBL | Displacement of [125I]echistatin from human placental integrin alphaVbeta3 receptor | B | 7.72 | pIC50 | 18.9 | nM | IC50 | Bioorg Med Chem (2008) 16: 4262-4271 [PMID:18343671] |
| ChEMBL | Displacement of [125I]-echistatin from alphavbeta3 integrin receptor | B | 7.72 | pIC50 | 18.9 | nM | IC50 | J Med Chem (2005) 48: 7675-7687 [PMID:16302808] |
| ChEMBL | Inhibition of vitronectin binding to recombinant human alphaV-beta3 integrin | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| ChEMBL | Binding affinity to Integrin alpha-v-beta-3 receptor by ELISA assay | B | 9.07 | pIC50 | 0.86 | nM | IC50 | Eur J Med Chem (2007) 42: 334-343 [PMID:17184884] |
| ChEMBL | Antagonist activity at alphavbeta3 integrin receptor (unknown origin) by cell-free ELISA | B | 9.19 | pIC50 | 0.65 | nM | IC50 | J Med Chem (2014) 57: 6301-6315 [PMID:24568695] |
| ChEMBL | Inhibition of integrin alphaVbeta3 | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of biotinylated ECM from human placental integrin alphavbeta3 receptor incubated for 3 hrs | B | 9.24 | pIC50 | 0.58 | nM | IC50 | Bioorg Med Chem (2016) 24: 989-994 [PMID:26818999] |
| ChEMBL | Binding affinity to human integrin alphaVbeta3 incubated for 1 hr by ELISA based solid phase integrin binding assay | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2021) 64: 586-601 [PMID:33356253] |
| ChEMBL | Inhibition of vitronectin binding to Integrin alphaVbeta3 receptor (unknown origin) by competitive ELISA | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2013) 56: 1509-1519 [PMID:23362923] |
| ChEMBL | Inhibition of vitronectin binding to human alphavbeta3 integrin receptor after 1 hr by competitive solid-phase binding ELISA | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2014) 57: 3410-3417 [PMID:24654918] |
| ChEMBL | Inhibition of vitronectin binding to human alphaVbeta3 integrin after 1 hr by ELISA | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2018) 61: 4791-4809 [PMID:29775303] |
| ChEMBL | Inhibition of human vitronectin binding to human integrin alphavbeta3 receptor after 1 hr by ELISA | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2019) 62: 7417-7430 [PMID:31306009] |
| ChEMBL | Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay | B | 9.27 | pIC50 | 0.54 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127039-127039 [PMID:32094009] |
| ChEMBL | Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay | B | 9.29 | pIC50 | 0.51 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6068-6072 [PMID:24095096] |
| ChEMBL | Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2 | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem (2016) 24: 703-711 [PMID:26753814] |
| integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/integrin, beta 5 subunit/Integrin alpha-V/beta-3/alpha-V/beta-5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106150] [GtoPdb: 2457, 2453, 2459] [UniProtKB: P05106, P06756, P18084] | ||||||||
| ChEMBL | Antagonist activity at integrin alphaVbeta3alphaVbeta5 (unknown origin) expressed in SKOV3 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1911-1913 [PMID:28351594] |
| integrin, alpha V subunit/integrin, beta 5 subunit/Integrin alpha-V/beta-5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096675] [GtoPdb: 2453, 2459] [UniProtKB: P06756, P18084] | ||||||||
| ChEMBL | Binding affinity to alphaVbeta5 integrin (unknown origin) | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Inhibition of vitronectin binding to human alphaVbeta5 integrin after 1 hr by ELISA | B | 5.27 | pIC50 | 5400 | nM | IC50 | J Med Chem (2014) 57: 5829-5834 [PMID:24949551] |
| ChEMBL | Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin | F | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| ChEMBL | Antagonist activity at integrin alphaVbeta5 (unknown origin) expressed in HT-29 cells assessed as reduction in cell adhesion to vitronectin after 2 hrs by MTT assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1911-1913 [PMID:28351594] |
| ChEMBL | Inhibition of vitronectin binding to recombinant human alphaV-beta5 integrin | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| ChEMBL | Antagonist activity at alphavbeta5 integrin receptor (unknown origin) by cell-free ELISA | B | 7.93 | pIC50 | 11.7 | nM | IC50 | J Med Chem (2014) 57: 6301-6315 [PMID:24568695] |
| ChEMBL | Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127039-127039 [PMID:32094009] |
| ChEMBL | Inhibition of vitronectin binding to Integrin alphaVbeta5 receptor (unknown origin) by competitive ELISA | B | 8.12 | pIC50 | 7.6 | nM | IC50 | J Med Chem (2013) 56: 1509-1519 [PMID:23362923] |
| ChEMBL | Binding affinity to Integrin alpha-v-beta-5 receptor by ELISA assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Eur J Med Chem (2007) 42: 334-343 [PMID:17184884] |
| ChEMBL | Displacement of [125I]Echistatin from human placental integrin alpha-V-beta-5 receptor | B | 9.89 | pIC50 | 0.13 | nM | IC50 | Bioorg Med Chem (2008) 16: 4262-4271 [PMID:18343671] |
| ChEMBL | Displacement of [125I]echistatin from human integrin alpha-V-beta-5 receptor by solid phase assay | B | 9.89 | pIC50 | 0.13 | nM | IC50 | J Med Chem (2008) 51: 1771-1782 [PMID:18303826] |
| ChEMBL | Displacement of [125I]echistatin from AlphaV-beta-5 integrin receptor | B | 9.89 | pIC50 | 0.13 | nM | IC50 | J Med Chem (2006) 49: 1808-1817 [PMID:16509596] |
| ChEMBL | Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor | B | 9.89 | pIC50 | 0.13 | nM | IC50 | J Med Chem (2005) 48: 7675-7687 [PMID:16302808] |
| integrin, alpha V subunit/integrin, beta 6 subunit/Integrin alpha-V/beta-6 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111416] [GtoPdb: 2453, 2460] [UniProtKB: P06756, P18564] | ||||||||
| ChEMBL | Inhibition of integrin alpha-v/beta-6 mediated UCLAP-3 cell adhesion to fibronectin | F | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| ChEMBL | Inhibition of latency-associated peptide binding to Integrin alphaVbeta6 receptor (unknown origin) by competitive ELISA | B | 5.78 | pIC50 | 1656 | nM | IC50 | J Med Chem (2013) 56: 1509-1519 [PMID:23362923] |
| ChEMBL | Inhibition of fibronectin binding to recombinant human alphaV-beta6 integrin | B | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (2002) 45: 1045-1051 [PMID:11855984] |
| integrin αVβ3 in Human [GtoPdb: 2583] | ||||||||
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - | J Med Chem (2002) 45: 1045-51 [PMID:11855984] |
ChEMBL data shown on this page come from version 33:
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]
