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Assay Detail

CHEMBL653843

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Binding
Kd (half effective concentration) of compound against CFTR (cystic fibrosis transmembrane conductance regulator) in rat was determined
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cystic fibrosis transmembrane conductance regulator (CHEMBL3992)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators.
Sammelson RE, Ma T, Galietta LJ, Verkman AS, Kurth MJ.
Bioorg Med Chem Lett (2003) 13 : 2509 -2512
PubMed 12852954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 22 4.25 4.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85369 1 4.64
CHEMBL44 GENISTEIN 2.0 1 4.40
CHEMBL81937 1 4.31
CHEMBL82279 1 4.30
CHEMBL81938 1 4.23
CHEMBL313066 1 4.21
CHEMBL312783 1 4.19
CHEMBL82409 1 4.18
CHEMBL82459 1 4.14
CHEMBL84391 1 4.14
CHEMBL309381 1 4.00
CHEMBL83374 1 -
CHEMBL82153 1 -
CHEMBL83050 1 -
CHEMBL313739 1 -
CHEMBL431213 1 -
CHEMBL310410 1 -
CHEMBL309839 1 -
CHEMBL83758 1 -
CHEMBL85504 1 -
CHEMBL310408 1 -
CHEMBL84000 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85369 Kd = 23000.0 nM 4.64
CHEMBL44 GENISTEIN Kd = 40000.0 nM 4.40
CHEMBL81937 Kd = 49000.0 nM 4.31
CHEMBL82279 Kd = 50000.0 nM 4.30
CHEMBL81938 Kd = 59000.0 nM 4.23
CHEMBL313066 Kd = 61000.0 nM 4.21
CHEMBL312783 Kd = 64000.0 nM 4.19
CHEMBL82409 Kd = 66000.0 nM 4.18
CHEMBL82459 Kd = 73000.0 nM 4.14
CHEMBL84391 Kd = 72000.0 nM 4.14
CHEMBL309381 Kd = 100000.0 nM 4.00
CHEMBL83374 Kd = 115000.0 nM -
CHEMBL82153 Kd = 110000.0 nM -
CHEMBL83050 Kd > 300000.0 nM -
CHEMBL313739 Kd = 118000.0 nM -
CHEMBL431213 Kd > 300000.0 nM -
CHEMBL310410 Kd = 177000.0 nM -
CHEMBL309839 Kd > 300000.0 nM -
CHEMBL83758 Kd = 220000.0 nM -
CHEMBL85504 Kd = 147000.0 nM -
CHEMBL310408 Kd = 104000.0 nM -
CHEMBL84000 Kd = 357000.0 nM -