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GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing
Date:10/25/2011

36

5.1 Introduction 36

5.1.1 Orphan GPCRs in the GRAFS Classification System 36

5.1.2 Orphan GPCRs in the Traditional Classification System 37

5.2 Current Methods Used in De-orphanization 38

5.2.1 Introduction 38

5.2.2 Reverse Pharmacology 39

5.2.3 Orphan Receptor Strategy 40

5.2.4 Phylogenetic Analysis and Chemogenomics 40

5.3 Functional Assays for De-orphanization 40

5.3.1 Introduction 40

5.3.2 G protein-dependent Assays 40

5.3.3 Recent G protein-independent Assays 41

6 GPCRs in Drug Discovery – Pipeline Analysis by Therapeutic Class 42

6.1 Central Nervous System 46

6.1.1 Introduction 46

6.1.2 Pipeline Profile 46

6.1.3 Major Indications 47

6.2 Oncology 52

6.2.1 Introduction 52

6.2.2 Pipeline Profile 52

6.2.3 Major Indications 53

6.3 Cardiovascular System 56

6.3.1 Introduction 56

6.3.2 Pipeline Profile 56

6.3.3 Major Indications 57

6.4 Metabolic Disorders 60

6.4.1 Introduction 60

6.4.2 Pipeline Profile 60

6.4.3 Major Indications 61

6.5 Gastrointestinal Disorders 64

6.5.1 Introduction 64

6.5.2 Pipeline Profile 64

6.5.3 Major Indications 65

6.6 Respiratory Diseases 67

6.6.1 Introduction 67

6.6.2 Pipeline Profile 67

6.6.3 Major Indications 68

6.7 Immunology 71

6.7.1 Introduction 71

6.7.2 Pipeline Profile 71

6.7.3 Major Indications 72

6.8 Women's Health 74

6.8.1 Introduction 74

6.8.2 Pipeline Profile 74

6.8.3 Major Indications 75

6.9 Ophthalmology 78

6.9.1 Introduction 78

6.9.2 Pipeline Profile 78

6.9.3 Major Indications 79

6.10 Genito-Urinary System and Sex Hormones 82

6.10.1 Introduction 82

6.10.2 Pipeline Profile 82

6.10.3 Major Indications 83

7 GPRCs in Drug Discovery – Pipeline Ana
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