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Assay Detail

CHEMBL4719920

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Binding
Binding affinity to HIV1 25-2AP TAR by 2-AP based fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of Small Molecules with a Noncanonical Binding Mode to HIV-1 Trans Activation Response (TAR) RNA.
Abulwerdi FA,Shortridge MD,Sztuba-Solinska J,Wilson R,Le Grice SF,Varani G,Schneekloth JS
J Med Chem (2016) 59 : 11148 -11160
PubMed 28002966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 4.27 4.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4797502 1 4.40
CHEMBL4750324 1 4.37
CHEMBL4793750 1 4.36
CHEMBL4776306 1 4.35
CHEMBL4747461 1 4.32
CHEMBL4474530 1 4.32
CHEMBL4779096 1 4.31
CHEMBL4750675 1 4.31
CHEMBL4745875 1 4.30
CHEMBL4778882 1 4.30
CHEMBL4782510 1 4.18
CHEMBL4764803 1 4.18
CHEMBL4776380 1 4.17
CHEMBL4797243 1 4.12
CHEMBL4748360 1 4.04
CHEMBL4762711 1 -
CHEMBL4751654 1 -
CHEMBL4800051 1 -
CHEMBL4744758 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4797502 Kd = 40000.0 nM 4.40
CHEMBL4750324 Kd = 42500.0 nM 4.37
CHEMBL4793750 Kd = 43300.0 nM 4.36
CHEMBL4776306 Kd = 44600.0 nM 4.35
CHEMBL4747461 Kd = 47700.0 nM 4.32
CHEMBL4474530 Kd = 47700.0 nM 4.32
CHEMBL4779096 Kd = 49100.0 nM 4.31
CHEMBL4750675 Kd = 48500.0 nM 4.31
CHEMBL4745875 Kd = 50300.0 nM 4.30
CHEMBL4778882 Kd = 50200.0 nM 4.30
CHEMBL4782510 Kd = 66400.0 nM 4.18
CHEMBL4764803 Kd = 66500.0 nM 4.18
CHEMBL4776380 Kd = 68000.0 nM 4.17
CHEMBL4797243 Kd = 75300.0 nM 4.12
CHEMBL4748360 Kd = 90100.0 nM 4.04
CHEMBL4762711 Kd > 400000.0 nM -
CHEMBL4751654 Kd > 400000.0 nM -
CHEMBL4800051 Kd > 400000.0 nM -
CHEMBL4744758 Kd > 400000.0 nM -