BDBM249277 US10017501, Compound 1020-18::US9458145, 1020-18

SMILES Cc1noc(C)c1-c1cc(-c2c(C)ccc3ncccc23)c2[nH]c(nc2c1)C1CC1

InChI Key InChIKey=KHQQNXFBTALTQF-UHFFFAOYSA-N

Data  3 KI  7 IC50  40 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 51 hits for monomerid = 249277   

TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKi:  3.80nMAssay Description:Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain2 after 60 mins by HTR...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKi:  7.5nMAssay Description:Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by HTR...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKi:  16nMAssay Description:Inhibition of tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [75-147](Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  87.1nMAssay Description:Binding of the two tandem bromodomains, BRD4-1 and BRD4-2, to an acetylated histone H4 peptide was measured using a homogeneous time resolved fluores...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  78.6nMAssay Description:Binding of the two tandem bromodomains, BRD4-1 and BRD4-2, to an acetylated histone H4 peptide was measured using a homogeneous time resolved fluores...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataEC50:  55nMAssay Description:Inhibition of BRD4 in human MM1S cells assessed as reduction in MYC transcription measured after 6 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  0.590nMAssay Description:Binding affinity to human partial length BRD2 bromodomain 2 isoform 1 (E348 to D455 residues) expressed in bacterial expression system after 1 hr by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 8(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  5.90E+3nMAssay Description:Binding affinity to BRD8 bromodomain 1 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone acetyltransferase p300(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  220nMAssay Description:Binding affinity to human partial length EP300 (A1040 to G1161 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription initiation factor TFIID subunit 1-like(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length TAF1L bromodomain 2 (Q1523 to D1654 residues) expressed in bacterial expression system after 1 hr by bromosc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATPase family AAA domain-containing protein 2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length ATAD2A (Q981 to R1108 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain adjacent to zinc finger domain protein 2A(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BAZ2A (M1792 to L1905 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain adjacent to zinc finger domain protein 2B(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BAZ2B (S2054 to S2168 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BRD1 (E556 to A688 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  1.70nMAssay Description:Binding affinity to human partial length BRD3 bromodomain 1 (P24 to E144 residues) expressed in bacterial expression system after 1 hr by bromoscan a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  0.660nMAssay Description:Binding affinity to BRD3 bromodomain 1/2 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  2.90nMAssay Description:Binding affinity to human partial length BRD4 bromodomain 1 long isoform (N44 to E168 residues) expressed in bacterial expression system after 1 hr b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  3.20nMAssay Description:Binding affinity to human partial length BRD4 bromodomain 2 long isoform (K333 to E460 residues) expressed in bacterial expression system after 1 hr ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 7(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 9(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BRD9 (R130 to V259 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  19nMAssay Description:Binding affinity to human partial length BRDT bromodomain 1 isoform b (N21 to E137 residues) expressed in bacterial expression system after 1 hr by b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  5nMAssay Description:Binding affinity to human partial length BRDT bromodomain 2 isoform b (K250 to E382 residues) expressed in bacterial expression system after 1 hr by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeregrin(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  4.10E+3nMAssay Description:Binding affinity to human partial length BRPF1 (E627 to G740 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChromatin remodeling regulator CECR2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  8.20E+3nMAssay Description:Binding affinity to human partial length CECR2 (P423 to D543 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone acetyltransferase KAT2A(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length GCN5L2 (E726 to K837 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein polybromo-1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length PBRM1 bromodomain 1 (S178 to E291 residues) expressed in bacterial expression system after 1 hr by bromoscan...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone acetyltransferase KAT2B(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length PCAF (G715 to D831 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription activator BRG1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length SMARCA4 (A1448 to S1575 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription initiation factor TFIID subunit 1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  8.00E+3nMAssay Description:Binding affinity to human partial length TAF1 bromodomain 2 (D1521 to D1656 residues) expressed in bacterial expression system after 1 hr by bromosca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription intermediary factor 1-alpha(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  6.90E+3nMAssay Description:Binding affinity to human partial length TRIM24 (P790 to P977 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain and WD repeat-containing protein 1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length WDR9 bromodomain 2 (A1310 to E1430 residues) expressed in bacterial expression system after 1 hr by bromosca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  1.10nMAssay Description:Binding affinity to BRD2 bromodomain 1/2 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  2.80nMAssay Description:Binding affinity to full length BRD4 short isoform (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain and PHD finger-containing protein 3(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length BRPF3 (E588 to G701 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProbable global transcription activator SNF2L2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length SMARCA2 (S1377 to Q1486 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  2.5nMAssay Description:Binding affinity to human partial length BRD2 bromodomain 1 long isoform (K71 to N194 residues) expressed in bacterial expression system after 1 hr b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  0.650nMAssay Description:Binding affinity to human partial length BRD3 bromodomain 2 (G306 to P416 residues) expressed in bacterial expression system after 1 hr by bromoscan ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 8(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to BRD8 bromodomain 2 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  4.90nMAssay Description:Binding affinity to BRDT bromodomain 1/2 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNucleosome-remodeling factor subunit BPTF(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length FALZ (S2791 to H2911 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein polybromo-1(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system after 1 hr by bromoscan...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription intermediary factor 1-alpha(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  4.10E+3nMAssay Description:Binding affinity to TRIM24 bromodomain (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  78nMAssay Description:Inhibition of biotin-labelled tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 br...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  83nMAssay Description:Inhibition of biotin-labelled tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 br...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATPase family AAA domain-containing protein 2B(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length ATAD2B (Q955 to R1082 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  1.30nMAssay Description:Binding affinity to BRD4 bromodomain 1/2 (unknown origin) after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCREB-binding protein(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd:  170nMAssay Description:Binding affinity to human partial length CREBBP (R1081 to G1197 residues) expressed in bacterial expression system after 1 hr by bromoscan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [75-147](Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  14.4nMpH: 7.5 T: 2°CAssay Description:Binding of the bromodomain BRD4-I to an acetylated histone H4 peptide was measured using a bead-based Amplified Luminescent Proximity Homogeneous Ass...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase TRIM33(Homo sapiens (Human))
Gilead Sciences

Curated by ChEMBL
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to human partial length TRIM33 PHD bromodomain (D882 to A1087 residues) expressed in bacterial expression system after 1 hr by bromo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [75-147](Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM249277(US10017501, Compound 1020-18 | US9458145, 1020-18)
Affinity DataIC50:  87.1nMpH: 7.5 T: 2°CAssay Description:Binding of the two tandem bromodomains, BRD4-1 and BRD4-2, to an acetylated histone H4 peptide was measured using a homogeneous time resolved fluores...More data for this Ligand-Target Pair
In DepthDetails US Patent
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