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Assay Detail

CHEMBL4681685

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

Binding
Inhibition of wild-type androgen receptor in human LAPC4 cells assessed as inhibition of DHT-induced luciferase activity measured after 24 hrs by luciferase reporter assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LAPC4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).
Wang C,Zhao Q,Vargas M,Jones JO,White KL,Shackleford DM,Chen G,Saunders J,Ng AC,Chiu FC,Dong Y,Charman SA,Keiser J,Vennerstrom JL
J Med Chem (2016) 59 : 10705 -10718
PubMed 27933964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.61 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4799175 1 6.85
CHEMBL4793070 1 6.58
CHEMBL4758277 1 6.54
CHEMBL1274 NILUTAMIDE 4.0 1 6.22
CHEMBL4787997 1 6.04
CHEMBL4755665 1 6.00
CHEMBL4750103 1 5.89
CHEMBL4778974 1 5.89
CHEMBL4778298 1 5.89
CHEMBL4790269 1 5.68
CHEMBL4786505 1 5.62
CHEMBL4786811 1 5.55
CHEMBL4572306 1 5.51
CHEMBL4778185 1 5.46
CHEMBL4799429 1 5.43
CHEMBL4782426 1 5.42
CHEMBL4747499 1 5.38
CHEMBL4743529 1 5.38
CHEMBL4748557 1 5.37
CHEMBL4465426 1 5.36
CHEMBL4748422 1 5.35
CHEMBL4793158 1 5.32
CHEMBL4763136 1 5.28
CHEMBL4781708 1 5.22
CHEMBL4740944 1 5.20
CHEMBL4777133 1 5.16
CHEMBL4777511 1 5.09
CHEMBL4746443 1 5.04
CHEMBL4763876 1 5.02
CHEMBL4779897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4799175 IC50 = 140.0 nM 6.85
CHEMBL4793070 IC50 = 260.0 nM 6.58
CHEMBL4758277 IC50 = 290.0 nM 6.54
CHEMBL1274 NILUTAMIDE IC50 = 600.0 nM 6.22
CHEMBL4787997 IC50 = 910.0 nM 6.04
CHEMBL4755665 IC50 = 990.0 nM 6.00
CHEMBL4750103 IC50 = 1300.0 nM 5.89
CHEMBL4778974 IC50 = 1300.0 nM 5.89
CHEMBL4778298 IC50 = 1300.0 nM 5.89
CHEMBL4790269 IC50 = 2100.0 nM 5.68
CHEMBL4786505 IC50 = 2400.0 nM 5.62
CHEMBL4786811 IC50 = 2800.0 nM 5.55
CHEMBL4572306 IC50 = 3100.0 nM 5.51
CHEMBL4778185 IC50 = 3500.0 nM 5.46
CHEMBL4799429 IC50 = 3700.0 nM 5.43
CHEMBL4782426 IC50 = 3800.0 nM 5.42
CHEMBL4747499 IC50 = 4200.0 nM 5.38
CHEMBL4743529 IC50 = 4200.0 nM 5.38
CHEMBL4748557 IC50 = 4300.0 nM 5.37
CHEMBL4465426 IC50 = 4400.0 nM 5.36
CHEMBL4748422 IC50 = 4500.0 nM 5.35
CHEMBL4793158 IC50 = 4800.0 nM 5.32
CHEMBL4763136 IC50 = 5300.0 nM 5.28
CHEMBL4781708 IC50 = 6000.0 nM 5.22
CHEMBL4740944 IC50 = 6300.0 nM 5.20
CHEMBL4777133 IC50 = 6900.0 nM 5.16
CHEMBL4777511 IC50 = 8100.0 nM 5.09
CHEMBL4746443 IC50 = 9100.0 nM 5.04
CHEMBL4763876 IC50 = 9600.0 nM 5.02
CHEMBL976 PRAZIQUANTEL IC50 - -
CHEMBL4795534 IC50 > 10000.0 nM -
CHEMBL4754845 IC50 > 10000.0 nM -
CHEMBL4782196 IC50 > 10000.0 nM -
CHEMBL4756377 IC50 > 10000.0 nM -
CHEMBL4744974 IC50 >= 10000.0 nM -
CHEMBL4747544 IC50 > 10000.0 nM -
CHEMBL4743225 IC50 > 10000.0 nM -
CHEMBL4779897 IC50 - -