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Assay Detail

CHEMBL4423291

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to recombinant human GR LBD by fluormone GS red-fluorescence polarization assay
ChEMBL ↗
47
Total Activities
47
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
Granberg KL, Yuan ZQ, Lindmark B, Edman K, Kajanus J, Hogner A, Malmgren M, O'Mahony G, Nordqvist A, Lindberg J, Tångefjord S, Kossenjans M, Löfberg C, Brånalt J, Liu D, Selmi N, Nikitidis G, Nordberg P, Hayen A, Aagaard A, Hansson E, Hermansson M, Ivarsson I, Jansson-Löfmark R, Karlsson U, Johansson U, William-Olsson L, Hartleib-Geschwindner J, Bamberg K.
J Med Chem (2019) 62 : 1385 -1406
PubMed 30596500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 6.56 8.90
pKi 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471322 — — 1 8.90
CHEMBL4463240 — — 1 8.80
CHEMBL4581588 — — 1 8.60
CHEMBL4555842 — — 1 8.10
CHEMBL4572476 — — 1 7.70
CHEMBL3918276 — — 1 7.50
CHEMBL4468672 — — 1 7.30
CHEMBL4440231 — — 1 7.10
CHEMBL4463035 — — 1 6.90
CHEMBL4573596 — — 1 6.90
CHEMBL4462110 — — 1 6.80
CHEMBL4448501 — — 1 6.70
CHEMBL4532472 — — 1 6.60
CHEMBL4483495 — — 1 6.50
CHEMBL4540313 — — 1 6.50
CHEMBL4544614 — — 1 6.50
CHEMBL4452144 — — 1 6.40
CHEMBL4442787 — — 1 6.20
CHEMBL4475012 — — 1 6.20
CHEMBL4556735 — — 1 6.00
CHEMBL4557356 — — 1 5.90
CHEMBL4557032 — — 1 5.90
CHEMBL4459932 — — 1 5.90
CHEMBL4455600 — — 1 5.90
CHEMBL4440099 — — 1 5.70
CHEMBL3916929 BALCINRENONE 3.0 1 5.60
CHEMBL4453801 — — 1 5.50
CHEMBL1095097 EPLERENONE 4.0 1 5.50
CHEMBL4519264 — — 1 5.30
CHEMBL4590259 — — 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471322 — Ki = 1.259 nM 8.90
CHEMBL4463240 — Ki = 1.585 nM 8.80
CHEMBL4581588 — Ki = 2.512 nM 8.60
CHEMBL4555842 — Ki = 7.943 nM 8.10
CHEMBL4572476 — Ki = 19.95 nM 7.70
CHEMBL3918276 — Ki = 31.62 nM 7.50
CHEMBL4468672 — Ki = 50.12 nM 7.30
CHEMBL4440231 — Ki = 79.43 nM 7.10
CHEMBL4463035 — Ki = 125.89 nM 6.90
CHEMBL4573596 — Ki = 125.89 nM 6.90
CHEMBL4462110 — Ki = 158.49 nM 6.80
CHEMBL4448501 — Ki = 199.53 nM 6.70
CHEMBL4532472 — Ki = 251.19 nM 6.60
CHEMBL4544614 — Ki = 316.23 nM 6.50
CHEMBL4540313 — Ki = 316.23 nM 6.50
CHEMBL4483495 — Ki = 316.23 nM 6.50
CHEMBL4452144 — Ki = 398.11 nM 6.40
CHEMBL4442787 — Ki = 630.96 nM 6.20
CHEMBL4475012 — Ki = 630.96 nM 6.20
CHEMBL4556735 — Ki = 1000.0 nM 6.00
CHEMBL4455600 — Ki = 1258.93 nM 5.90
CHEMBL4459932 — Ki = 1258.93 nM 5.90
CHEMBL4557356 — Ki = 1258.93 nM 5.90
CHEMBL4557032 — Ki = 1258.93 nM 5.90
CHEMBL4440099 — Ki = 1995.26 nM 5.70
CHEMBL3916929 BALCINRENONE Ki = 2511.89 nM 5.60
CHEMBL4453801 — Ki = 3162.28 nM 5.50
CHEMBL1095097 EPLERENONE Ki = 3162.28 nM 5.50
CHEMBL4519264 — Ki = 5011.87 nM 5.30
CHEMBL4590259 — Ki = 6309.57 nM 5.20
CHEMBL4446086 — Ki = 12589.25 nM 4.90
CHEMBL4528177 — Ki > 12589.25 nM -
CHEMBL4560632 — Ki > 15848.93 nM -
CHEMBL4470069 — pKi - — -
CHEMBL4474698 — Ki > 12589.25 nM -
CHEMBL4470268 — Ki > 15848.93 nM -
CHEMBL4474881 — pKi - — -
CHEMBL4580706 — pKi - — -
CHEMBL4473402 — pKi - — -
CHEMBL4445440 — Ki > 15848.93 nM -
CHEMBL4446088 — Ki > 15848.93 nM -
CHEMBL4588402 — Ki > 15848.93 nM -
CHEMBL4566513 — pKi - — -
CHEMBL4462225 — pKi - — -
CHEMBL4463126 — Ki > 15848.93 nM -
CHEMBL4539557 — pKi - — -
CHEMBL4585636 — Ki > 15848.93 nM -