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Assay Detail

CHEMBL4423293

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

Binding
Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene 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
IC50 52 6.61 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463240 — — 1 9.10
CHEMBL4471322 — — 1 8.60
CHEMBL4572476 — — 1 8.60
CHEMBL4555842 — — 1 7.70
CHEMBL4532472 — — 1 7.60
CHEMBL1393 SPIRONOLACTONE 4.0 1 7.30
CHEMBL3775714 — — 1 7.30
CHEMBL3918276 — — 1 7.30
CHEMBL4573596 — — 1 7.30
CHEMBL4468672 — — 1 7.20
CHEMBL4556735 — — 1 7.20
CHEMBL4452144 — — 1 7.10
CHEMBL4581588 — — 1 7.10
CHEMBL4540313 — — 1 7.10
CHEMBL4463035 — — 1 7.00
CHEMBL4483495 — — 1 7.00
CHEMBL4544614 — — 1 6.90
CHEMBL2181928 — — 1 6.70
CHEMBL4557356 — — 1 6.70
CHEMBL4440231 — — 1 6.70
CHEMBL4442787 — — 1 6.60
CHEMBL4448501 — — 1 6.60
CHEMBL4566513 — — 1 6.50
CHEMBL3916929 BALCINRENONE 3.0 1 6.40
CHEMBL4459932 — — 1 6.30
CHEMBL4453801 — — 1 6.20
CHEMBL4475012 — — 1 6.20
CHEMBL4455600 — — 1 6.20
CHEMBL1095097 EPLERENONE 4.0 1 6.10
CHEMBL4440099 — — 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463240 — IC50 = 0.7943 nM 9.10
CHEMBL4471322 — IC50 = 2.512 nM 8.60
CHEMBL4572476 — IC50 = 2.512 nM 8.60
CHEMBL4555842 — IC50 = 19.95 nM 7.70
CHEMBL4532472 — IC50 = 25.12 nM 7.60
CHEMBL1393 SPIRONOLACTONE IC50 = 50.12 nM 7.30
CHEMBL3775714 — IC50 = 50.12 nM 7.30
CHEMBL3918276 — IC50 = 50.12 nM 7.30
CHEMBL4573596 — IC50 = 50.12 nM 7.30
CHEMBL4468672 — IC50 = 63.1 nM 7.20
CHEMBL4556735 — IC50 = 63.1 nM 7.20
CHEMBL4540313 — IC50 = 79.43 nM 7.10
CHEMBL4581588 — IC50 = 79.43 nM 7.10
CHEMBL4452144 — IC50 = 79.43 nM 7.10
CHEMBL4483495 — IC50 = 100.0 nM 7.00
CHEMBL4463035 — IC50 = 100.0 nM 7.00
CHEMBL4544614 — IC50 = 125.89 nM 6.90
CHEMBL2181928 — IC50 = 199.53 nM 6.70
CHEMBL4557356 — IC50 = 199.53 nM 6.70
CHEMBL4440231 — IC50 = 199.53 nM 6.70
CHEMBL4442787 — IC50 = 251.19 nM 6.60
CHEMBL4448501 — IC50 = 251.19 nM 6.60
CHEMBL4566513 — IC50 = 316.23 nM 6.50
CHEMBL3916929 BALCINRENONE IC50 = 398.11 nM 6.40
CHEMBL4459932 — IC50 = 501.19 nM 6.30
CHEMBL4453801 — IC50 = 630.96 nM 6.20
CHEMBL4455600 — IC50 = 630.96 nM 6.20
CHEMBL4475012 — IC50 = 630.96 nM 6.20
CHEMBL1095097 EPLERENONE IC50 = 794.33 nM 6.10
CHEMBL4440099 — IC50 = 794.33 nM 6.10
CHEMBL4462110 — IC50 = 1000.0 nM 6.00
CHEMBL4557032 — IC50 = 1000.0 nM 6.00
CHEMBL4474881 — IC50 = 1584.89 nM 5.80
CHEMBL4580706 — IC50 = 1995.26 nM 5.70
CHEMBL4474698 — IC50 = 1995.26 nM 5.70
CHEMBL4590259 — IC50 = 1995.26 nM 5.70
CHEMBL4446086 — IC50 = 2511.89 nM 5.60
CHEMBL4473402 — IC50 = 3162.28 nM 5.50
CHEMBL4462225 — IC50 = 3981.07 nM 5.40
CHEMBL4467010 — IC50 = 5011.87 nM 5.30
CHEMBL4445438 — IC50 = 6309.57 nM 5.20
CHEMBL4528177 — IC50 = 6309.57 nM 5.20
CHEMBL4539557 — IC50 > 10000.0 nM -
CHEMBL4585636 — IC50 > 10000.0 nM -
CHEMBL4445440 — IC50 > 10000.0 nM -
CHEMBL4463126 — IC50 > 10000.0 nM -
CHEMBL4446088 — IC50 > 10000.0 nM -
CHEMBL4519264 — IC50 > 10000.0 nM -
CHEMBL4470268 — IC50 > 10000.0 nM -
CHEMBL4588402 — IC50 > 10000.0 nM -