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Assay Detail

CHEMBL925405

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

Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.
Corbett JW, Rauckhorst MR, Qian F, Hoffman RL, Knauer CS, Fitzgerald LW.
Bioorg Med Chem Lett (2007) 17 : 6250 -6256
PubMed 17888659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 62 6.41 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398531 1 7.96
CHEMBL248785 1 7.66
CHEMBL251200 1 7.66
CHEMBL398258 1 7.52
CHEMBL250282 1 7.46
CHEMBL248996 1 7.29
CHEMBL250814 1 7.28
CHEMBL248803 1 7.24
CHEMBL250617 1 7.23
CHEMBL250815 1 7.17
CHEMBL400082 1 7.09
CHEMBL250616 1 6.94
CHEMBL398843 1 6.67
CHEMBL251397 1 6.65
CHEMBL401327 1 6.60
CHEMBL398425 1 6.58
CHEMBL249430 1 6.47
CHEMBL250618 1 6.42
CHEMBL401295 1 6.40
CHEMBL251199 1 6.36
CHEMBL402717 1 6.34
CHEMBL430019 1 6.33
CHEMBL400156 1 6.29
CHEMBL449657 1 6.28
CHEMBL400154 1 6.15
CHEMBL250615 1 5.93
CHEMBL249212 1 5.92
CHEMBL400155 1 5.92
CHEMBL251006 1 5.92
CHEMBL248577 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398531 Ki = 11.0 nM 7.96
CHEMBL248785 Ki = 22.0 nM 7.66
CHEMBL251200 Ki = 22.0 nM 7.66
CHEMBL398258 Ki = 30.0 nM 7.52
CHEMBL250282 Ki = 35.0 nM 7.46
CHEMBL248996 Ki = 51.0 nM 7.29
CHEMBL250814 Ki = 53.0 nM 7.28
CHEMBL248803 Ki = 58.0 nM 7.24
CHEMBL250617 Ki = 59.0 nM 7.23
CHEMBL250815 Ki = 67.0 nM 7.17
CHEMBL400082 Ki = 82.0 nM 7.09
CHEMBL250616 Ki = 115.0 nM 6.94
CHEMBL398843 Ki = 214.0 nM 6.67
CHEMBL251397 Ki = 222.0 nM 6.65
CHEMBL401327 Ki = 251.0 nM 6.60
CHEMBL398425 Ki = 266.0 nM 6.58
CHEMBL249430 Ki = 337.0 nM 6.47
CHEMBL250618 Ki = 384.0 nM 6.42
CHEMBL401295 Ki = 401.0 nM 6.40
CHEMBL251199 Ki = 436.0 nM 6.36
CHEMBL402717 Ki = 456.0 nM 6.34
CHEMBL430019 Ki = 472.0 nM 6.33
CHEMBL400156 Ki = 509.0 nM 6.29
CHEMBL449657 Ki = 530.0 nM 6.28
CHEMBL400154 Ki = 711.0 nM 6.15
CHEMBL250615 Ki = 1185.0 nM 5.93
CHEMBL400155 Ki = 1207.0 nM 5.92
CHEMBL251006 Ki = 1217.0 nM 5.92
CHEMBL249212 Ki = 1208.0 nM 5.92
CHEMBL248577 Ki = 1261.0 nM 5.90
CHEMBL248585 Ki = 1540.0 nM 5.81
CHEMBL400952 Ki = 1733.0 nM 5.76
CHEMBL251034 Ki = 2021.0 nM 5.69
CHEMBL248623 Ki = 2123.0 nM 5.67
CHEMBL398300 Ki = 2376.0 nM 5.62
CHEMBL248816 Ki = 2434.0 nM 5.61
CHEMBL248588 Ki = 2703.0 nM 5.57
CHEMBL400531 Ki = 3382.0 nM 5.47
CHEMBL249191 Ki = 3980.0 nM 5.40
CHEMBL249012 Ki = 4688.0 nM 5.33
CHEMBL399877 Ki = 5473.0 nM 5.26
CHEMBL251204 Ki > 10000.0 nM -
CHEMBL248784 Ki > 10000.0 nM -
CHEMBL251007 Ki > 10000.0 nM -
CHEMBL398365 Ki > 10000.0 nM -
CHEMBL250653 Ki > 10000.0 nM -
CHEMBL399936 Ki > 10000.0 nM -
CHEMBL251198 Ki > 10000.0 nM -
CHEMBL250680 Ki > 10000.0 nM -
CHEMBL401297 Ki > 10000.0 nM -