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Assay Detail

CHEMBL4423290

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

Binding
Displacement of [3H]-aldosterone to human mineralocorticoid receptor LBD by radiometric binding assay
ChEMBL ↗
52
Total Activities
52
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

Mineralocorticoid receptor (CHEMBL1994) ↗
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 52 7.37 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4572476 — — 1 9.50
CHEMBL4471322 — — 1 9.30
CHEMBL4555842 — — 1 9.20
CHEMBL4532472 — — 1 9.10
CHEMBL4468672 — — 1 8.70
CHEMBL4573596 — — 1 8.60
CHEMBL4581588 — — 1 8.50
CHEMBL4540313 — — 1 8.50
CHEMBL3918276 — — 1 8.40
CHEMBL4483495 — — 1 8.40
CHEMBL1393 SPIRONOLACTONE 4.0 1 8.30
CHEMBL4463035 — — 1 8.10
CHEMBL4544614 — — 1 8.10
CHEMBL4448501 — — 1 8.00
CHEMBL4440231 — — 1 8.00
CHEMBL4452144 — — 1 7.90
CHEMBL3775714 — — 1 7.90
CHEMBL4556735 — — 1 7.80
CHEMBL2181928 — — 1 7.60
CHEMBL4557356 — — 1 7.40
CHEMBL3916929 BALCINRENONE 3.0 1 7.40
CHEMBL4453801 — — 1 7.30
CHEMBL4442787 — — 1 7.30
CHEMBL4475012 — — 1 7.20
CHEMBL4566513 — — 1 7.20
CHEMBL4462110 — — 1 7.00
CHEMBL4455600 — — 1 7.00
CHEMBL4440099 — — 1 6.90
CHEMBL1095097 EPLERENONE 4.0 1 6.90
CHEMBL4557032 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4572476 — Ki = 0.3162 nM 9.50
CHEMBL4471322 — Ki = 0.5012 nM 9.30
CHEMBL4555842 — Ki = 0.631 nM 9.20
CHEMBL4532472 — Ki = 0.7943 nM 9.10
CHEMBL4468672 — Ki = 1.995 nM 8.70
CHEMBL4573596 — Ki = 2.512 nM 8.60
CHEMBL4581588 — Ki = 3.162 nM 8.50
CHEMBL4540313 — Ki = 3.162 nM 8.50
CHEMBL3918276 — Ki = 3.981 nM 8.40
CHEMBL4483495 — Ki = 3.981 nM 8.40
CHEMBL1393 SPIRONOLACTONE Ki = 5.012 nM 8.30
CHEMBL4463035 — Ki = 7.943 nM 8.10
CHEMBL4544614 — Ki = 7.943 nM 8.10
CHEMBL4440231 — Ki = 10.0 nM 8.00
CHEMBL4448501 — Ki = 10.0 nM 8.00
CHEMBL4452144 — Ki = 12.59 nM 7.90
CHEMBL3775714 — Ki = 12.59 nM 7.90
CHEMBL4556735 — Ki = 15.85 nM 7.80
CHEMBL2181928 — Ki = 25.12 nM 7.60
CHEMBL4557356 — Ki = 39.81 nM 7.40
CHEMBL3916929 BALCINRENONE Ki = 39.81 nM 7.40
CHEMBL4453801 — Ki = 50.12 nM 7.30
CHEMBL4442787 — Ki = 50.12 nM 7.30
CHEMBL4475012 — Ki = 63.1 nM 7.20
CHEMBL4566513 — Ki = 63.1 nM 7.20
CHEMBL4462110 — Ki = 100.0 nM 7.00
CHEMBL4455600 — Ki = 100.0 nM 7.00
CHEMBL4440099 — Ki = 125.89 nM 6.90
CHEMBL1095097 EPLERENONE Ki = 125.89 nM 6.90
CHEMBL4557032 — Ki = 158.49 nM 6.80
CHEMBL4519264 — Ki = 158.49 nM 6.80
CHEMBL4459932 — Ki = 199.53 nM 6.70
CHEMBL4590259 — Ki = 316.23 nM 6.50
CHEMBL4474698 — Ki = 398.11 nM 6.40
CHEMBL4577956 — Ki = 501.19 nM 6.30
CHEMBL4462225 — Ki = 501.19 nM 6.30
CHEMBL4580706 — Ki = 630.96 nM 6.20
CHEMBL4474881 — Ki = 794.33 nM 6.10
CHEMBL4528177 — Ki = 1000.0 nM 6.00
CHEMBL4446086 — Ki = 1000.0 nM 6.00
CHEMBL4473402 — Ki = 1000.0 nM 6.00
CHEMBL4446088 — Ki = 1258.93 nM 5.90
CHEMBL4467010 — Ki = 1995.26 nM 5.70
CHEMBL4539557 — Ki = 6309.57 nM 5.20
CHEMBL4463126 — Ki > 10000.0 nM -
CHEMBL4588402 — Ki > 10000.0 nM -
CHEMBL4463240 — Ki < 0.3162 nM -
CHEMBL4585636 — Ki > 6309.57 nM -
CHEMBL4445440 — Ki > 10000.0 nM -
CHEMBL4560632 — Ki > 10000.0 nM -