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| Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Bromodomain-containing protein 4 [44-168] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet  | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 21 | n/a | n/a | n/a | n/a | 7.5 | 25 |
Dana-Farber Cancer Institute | Assay Description Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150... | Nat Chem Biol 12: 1089-1096 (2016) Article DOI: 10.1038/nchembio.2209 BindingDB Entry DOI: 10.7270/Q2VQ31HW | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [44-167] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB MMDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 29 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were dil... | Citation and Details BindingDB Entry DOI: 10.7270/Q2833W75 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [44-167] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB MMDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 29 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Acetyl-Histone Binding Assay. Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElme... | Citation and Details BindingDB Entry DOI: 10.7270/Q20K2CS3 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 33 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of human His-tagged BRD4 bromodomain2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00960 BindingDB Entry DOI: 10.7270/Q29W0K46 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 2 [364-436] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 52 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [342-460] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 62 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 3 [326-398] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 69 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain testis-specific protein [22-138] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 77 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were dil... | Citation and Details BindingDB Entry DOI: 10.7270/Q2833W75 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain testis-specific protein [22-138] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 77 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Acetyl-Histone Binding Assay. Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElme... | Citation and Details BindingDB Entry DOI: 10.7270/Q20K2CS3 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 77 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of human His-tagged BRD4 bromodomain1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00960 BindingDB Entry DOI: 10.7270/Q29W0K46 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 2 [91-163] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 78 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 3 [51-123] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 81 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [49-170] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 92 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain testis-specific protein [22-138] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 183 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain testis-specific protein [287-359] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 217 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | US11890288, Compound (+)-JQ1 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | n/a | n/a | 550 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details | ||||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 550 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Table 4-2: The inhibitory action of the compound of the present invention on the binding of BRD4 protein and a ligand thereof (acetylated histone H4)... | Citation and Details BindingDB Entry DOI: 10.7270/Q2MW2N0S | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 7.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Table 4-1: The inhibitory action of the compound of the present invention on the binding of BRD4 protein and a ligand thereof was evaluated by the ti... | Citation and Details BindingDB Entry DOI: 10.7270/Q2MW2N0S | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Isoform C of Bromodomain-containing protein 4 (Short) (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 7.76E+3 | n/a | n/a | n/a | n/a | 7.5 | 25 |
Dana-Farber Cancer Institute | Assay Description Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150... | Nat Chem Biol 12: 1089-1096 (2016) Article DOI: 10.1038/nchembio.2209 BindingDB Entry DOI: 10.7270/Q2VQ31HW | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| CREB-binding protein (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 9.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,... | Citation and Details BindingDB Entry DOI: 10.7270/Q2TT4V40 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [44-167] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB MMDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 8.35E+6 | n/a | n/a | n/a | n/a | n/a | n/a |
Tensha Therapeutics, Inc. US Patent | Assay Description The binding activity of lead compounds with the BRD4 site 1 was determined by Alpha-assay with a 12-point dose response curve | US Patent US10925881 (2021) BindingDB Entry DOI: 10.7270/Q2JS9TJ1 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [75-147] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 8.35E+6 | n/a | n/a | n/a | n/a | n/a | n/a |
Dana-Farber Cancer Institute, Inc. US Patent | Assay Description All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature ... | US Patent US10407441 (2019) BindingDB Entry DOI: 10.7270/Q2RJ4MV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 8.35E+6 | n/a | n/a | n/a | n/a | 7.4 | 25 |
DANA-FARBER CANCER INSTITUTE, INC. US Patent | Assay Description BRD4(1): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer... | US Patent US9320741 (2016) BindingDB Entry DOI: 10.7270/Q2KP811P | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [349-460] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 5.21E+7 | n/a | n/a | n/a | n/a | n/a | n/a |
Tensha Therapeutics, Inc. US Patent | Assay Description The binding activity of lead compounds with the BRD4 site 2 was determined by Alpha-assay with a 12-point dose response curve | US Patent US10925881 (2021) BindingDB Entry DOI: 10.7270/Q2JS9TJ1 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 [368-440] (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 5.21E+7 | n/a | n/a | n/a | n/a | n/a | n/a |
Dana-Farber Cancer Institute, Inc. US Patent | Assay Description All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature ... | US Patent US10407441 (2019) BindingDB Entry DOI: 10.7270/Q2RJ4MV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Bromodomain-containing protein 4 (Homo sapiens (Human)) | BDBM205429 ( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 5.21E+7 | n/a | n/a | n/a | n/a | 7.4 | 25 |
DANA-FARBER CANCER INSTITUTE, INC. US Patent | Assay Description BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer... | US Patent US9320741 (2016) BindingDB Entry DOI: 10.7270/Q2KP811P | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
