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Assay Detail

CHEMBL5368301

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Binding
Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein polybromo-1 (CHEMBL1795184)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1.
Cochran AG, Flynn M.
J Med Chem (2023) 66 : 13116 -13134
PubMed 37702400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 26 6.99 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5415064 1 8.22
CHEMBL5412292 1 8.05
CHEMBL5424811 1 8.00
CHEMBL5409404 1 7.72
CHEMBL5401472 1 7.66
CHEMBL5406315 1 7.62
CHEMBL5398829 1 7.54
CHEMBL5431862 1 7.44
CHEMBL5177096 1 7.40
CHEMBL5411199 1 7.40
CHEMBL5428009 1 7.40
CHEMBL5425250 1 7.28
CHEMBL5396881 1 5.40
CHEMBL5394310 1 4.96
CHEMBL5426305 1 4.89
CHEMBL5421138 1 4.82
CHEMBL5399079 1 -
CHEMBL5402159 1 -
CHEMBL5395676 1 -
CHEMBL5406457 1 -
CHEMBL5415837 1 -
CHEMBL5401735 1 -
CHEMBL5431005 1 -
CHEMBL5441040 1 -
CHEMBL5415253 1 -
CHEMBL5415396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5415064 Kd = 6.0 nM 8.22
CHEMBL5412292 Kd = 9.0 nM 8.05
CHEMBL5424811 Kd = 10.0 nM 8.00
CHEMBL5409404 Kd = 19.0 nM 7.72
CHEMBL5401472 Kd = 22.0 nM 7.66
CHEMBL5406315 Kd = 24.0 nM 7.62
CHEMBL5398829 Kd = 29.0 nM 7.54
CHEMBL5431862 Kd = 36.0 nM 7.44
CHEMBL5177096 Kd = 40.0 nM 7.40
CHEMBL5411199 Kd = 40.0 nM 7.40
CHEMBL5428009 Kd = 40.0 nM 7.40
CHEMBL5425250 Kd = 53.0 nM 7.28
CHEMBL5396881 Kd = 3950.0 nM 5.40
CHEMBL5394310 Kd = 11000.0 nM 4.96
CHEMBL5426305 Kd = 13000.0 nM 4.89
CHEMBL5421138 Kd = 15000.0 nM 4.82
CHEMBL5399079 Kd > 20000.0 nM -
CHEMBL5402159 Kd > 20000.0 nM -
CHEMBL5395676 Kd > 10000.0 nM -
CHEMBL5406457 Kd > 20000.0 nM -
CHEMBL5415837 Kd > 10000.0 nM -
CHEMBL5401735 Kd > 10000.0 nM -
CHEMBL5431005 Kd > 20000.0 nM -
CHEMBL5441040 Kd > 20000.0 nM -
CHEMBL5415253 Kd > 20000.0 nM -
CHEMBL5415396 Kd > 20000.0 nM -